Assay ID | Title | Year | Journal | Article |
AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1470601 | Cytotoxicity against human HT-29 cells pretreated for 24 hrs under normoxic condition followed by compound washout measured after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38. |
AID1593650 | Cytotoxicity against human HL60 cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives. |
AID1703229 | Solubility of compound in phosphate buffer at pH 7.4 incubated for 24 hrs under shaking condition by HPLC analysis | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID249952 | In vitro cytotoxic activity against human RPM12650 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1666200 | Cytotoxicity against human 16HBE cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging. |
AID1655976 | Cytotoxicity against human SK-MEL-24 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Artemisinin Derivatives with Antimelanoma Activity Show Inhibitory Effect against Human DNA Topoisomerase 1. |
AID666765 | Inhibition of topo 1-mediated relaxation of supercoiled pBR322 at 10 to 100 uM after 30 mins using ethidium bromide by agarose-gel electrophoresis | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and biological evaluation of new homocamptothecin analogs. |
AID624633 | Drug glucuronidation reaction catalyzed by human recombinant UGT1A4 | 2005 | Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
| UDP-glucuronosyltransferases and clinical drug-drug interactions. |
AID249906 | In vitro cytotoxic activity against human T24 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID624638 | Drug glucuronidation reaction catalyzed by human recombinant UGT2B15 | 2005 | Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
| UDP-glucuronosyltransferases and clinical drug-drug interactions. |
AID1708532 | Growth inhibition of human NCI-H226 cells by Cell-titer96 assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| Copper(I)-Catalyzed Nitrile-Addition/ |
AID321558 | Antiproliferative activity against human DU145 cells after 96 hrs | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Synthesis and bioevaluation of 22-hydroxyacuminatine analogs. |
AID624630 | Drug glucuronidation reaction catalyzed by human recombinant UGT1A1 | 2005 | Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
| UDP-glucuronosyltransferases and clinical drug-drug interactions. |
AID84434 | Antiproliferative activity against human HT-29 colon cell line | 1999 | Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17
| BN 80927: a novel homocamptothecin with inhibitory activities on both topoisomerase I and topoisomerase II. |
AID1215101 | Terminal elimination rate constant in cancer patient normal renal function administered as infusion after 0.25 to 1.5 hrs by RP-HPLC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Delayed elimination of SN-38 in cancer patients with severe renal failure. |
AID249937 | In vitro cytotoxic activity against human Hs 174.T cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1626189 | Synergistic cytotoxicity in human HT-29 cells assessed as dose reduction index ratio in presence of CoCl2-induced hypoxic conditions measured at 80 % cell growth inhibition after 72 hrs in presence of compound-5c by cell counter method | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| 1,2-Benzisothiazole Derivatives Bearing 4-, 5-, or 6-Alkyl/arylcarboxamide Moieties Inhibit Carbonic Anhydrase Isoform IX (CAIX) and Cell Proliferation under Hypoxic Conditions. |
AID247883 | Concentration required to inhibit growth of human prostate PC-3 carcinoma cell line | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
| Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction. |
AID216612 | Antitumor activity against MTW0 WiDr xenografts in nude mice at a dose of 10 umol/kg | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
| Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues. |
AID679163 | TP_TRANSPORTER: uptake in OATP1B1-expressing HEK293 cell | 2005 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 33, Issue:3
| Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms. |
AID414759 | Cytotoxicity against MDR1 overexpressing human KBV1 cells after 4 days by MTT method | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
| 12-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridines as novel topoisomerase I-targeting antitumor agents. |
AID589114 | Mechanism based inhibition of human cytochrome P450 3A4 | 2005 | Current drug metabolism, Oct, Volume: 6, Issue:5
| Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. |
AID248673 | In-vitro inhibitory concentration for human tumor HELA cell-line was determined using MTT assay after 3 days of incubation | 2005 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
| Synthesis and antitumor activity of the hexacyclic camptothecin derivatives. |
AID418333 | Antiproliferative activity against human NCI-H460 cells after 3 days | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| Synthesis of new camptothecin analogs with improved antitumor activities. |
AID679412 | TP_TRANSPORTER: uptake of SN-38 at a concentration of 0.10uL/oocyte in Xenopus laevis oocytes | 2005 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 33, Issue:3
| Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms. |
AID1194773 | Stability in human plasma assessed as lactone moieties level at 1 uM incubated at 37 degC after 3 hrs by HPLC method | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
| Design, synthesis and biological evaluation of novel homocamptothecin analogues as potent antitumor agents. |
AID1754555 | Cytotoxicity against human CCD-841CoN cells assessed as inhibition of cell growth measured after 72 hrs | 2021 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 46 | New camptothecin derivatives for generalized oncological chemotherapy: Synthesis, stereochemistry and biology. |
AID679173 | TP_TRANSPORTER: drug resistance in BCRP-expressing K562 cells | 2003 | Molecular cancer therapeutics, Jan, Volume: 2, Issue:1
| Reversal of breast cancer resistance protein-mediated drug resistance by estrogen antagonists and agonists. |
AID249916 | In vitro cytotoxic activity against human T98G cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID249935 | In vitro cytotoxic activity against human HT144 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID26144 | Half-life in PBS buffer solution in the absence of human serum albumin | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
| The structural basis of camptothecin interactions with human serum albumin: impact on drug stability. |
AID745327 | Cytotoxicity against human DU145 cells | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents. |
AID28882 | Half life of compound in PBS suspension | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity. |
AID1222390 | Drug metabolism assessed as UGT1A1 (unknown origin)-mediated compound glucuronidation | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Correlation between bilirubin glucuronidation and estradiol-3-gluronidation in the presence of model UDP-glucuronosyltransferase 1A1 substrates/inhibitors. |
AID1754554 | Cytotoxicity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs | 2021 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 46 | New camptothecin derivatives for generalized oncological chemotherapy: Synthesis, stereochemistry and biology. |
AID680997 | TP_TRANSPORTER: inhibition of E1S uptake by 7-ethyl-10-hydroxycamptothecin at a concentration of 20uM in membrane vesicle from BCRP-expressing K562 cells | 2003 | Molecular pharmacology, Sep, Volume: 64, Issue:3
| Breast cancer resistance protein exports sulfated estrogens but not free estrogens. |
AID426062 | Antitumor activity against human A549/ATCC cells by SRB method | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| 7-Cycloalkylcamptothecin derivatives: Preparation and biological evaluation. |
AID321560 | Antiproliferative activity against human HT29 cells after 96 hrs | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Synthesis and bioevaluation of 22-hydroxyacuminatine analogs. |
AID1465633 | Cmax in Beagle dog at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle. |
AID678965 | TP_TRANSPORTER: drug resistance in BCRP-expressing PA317 cells | 2003 | International journal of cancer, Dec-10, Volume: 107, Issue:5
| Single amino acid substitutions in the transmembrane domains of breast cancer resistance protein (BCRP) alter cross resistance patterns in transfectants. |
AID749703 | Inhibition of HDAC6 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Dual-acting histone deacetylase-topoisomerase I inhibitors. |
AID1561988 | Drug uptake in human A549 cells assessed as blue fluorescence at 5 uM after 12 hrs by confocal laser scanning microscopic analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
AID678800 | TP_TRANSPORTER: increase of cytotoxicity by GF120918 in MX3 cells | 2001 | Clinical cancer research : an official journal of the American Association for Cancer Research, Apr, Volume: 7, Issue:4
| Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918. |
AID1703210 | Cytotoxicity against human A549 assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID1386601 | Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay | 2018 | Journal of natural products, 09-28, Volume: 81, Issue:9
| Flabellipparicine, a Flabelliformide-Apparicine-Type Bisindole Alkaloid from Tabernaemontana divaricata. |
AID249946 | In vitro cytotoxic activity against human Capan-2 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID247623 | Inhibitory concentration against human HCT116 colon cancer cell line | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
| Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin. |
AID249956 | In vitro cytotoxic activity against human Su.86.86 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1561986 | Drug uptake in human A549 cells assessed as blue shift in absorption spectrum at 5 uM by UV-visible absorption spectral analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
AID28493 | % lactone at different intervals of time in PBS with RBC suspension | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity. |
AID594370 | Cytotoxicity against human A549 cells | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Semisynthesis of triptolide analogues: effect of γ-lactone and C-14 substituents on cytotoxic activities. |
AID27450 | Half-life period in human plasma | 1993 | Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
| Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin. |
AID1708541 | Resistance index, ratio of GI50 for growth inhibition of ARC-111-resistant human HA6n cells to GI50 for growth inhibition of human HCT-116 cells | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| Copper(I)-Catalyzed Nitrile-Addition/ |
AID1076087 | Cytotoxicity against human HCT116 cells | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
| Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs. |
AID227859 | In Vitro cytotoxicity against human stomach cancer cell line (MKN45) | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
| Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues. |
AID26145 | Half-life in PBS buffer solution in the presence of human serum albumin | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
| The structural basis of camptothecin interactions with human serum albumin: impact on drug stability. |
AID1294917 | Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | 10-Boronic acid substituted camptothecin as prodrug of SN-38. |
AID27446 | Half-life period in HSA buffer at 37 C in the presence of human serum albumin | 1993 | Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
| Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin. |
AID1515334 | Antiproliferative activity against human U251 cells after 48 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
| Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold. |
AID234607 | Tested for (median survival time of treated/control animals) x100 at dosage of 30 mg/kg. | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Antitumor agents. 7. Synthesis and antitumor activity of novel hexacyclic camptothecin analogues. |
AID1655974 | Cytotoxicity against human C3PV cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Artemisinin Derivatives with Antimelanoma Activity Show Inhibitory Effect against Human DNA Topoisomerase 1. |
AID679982 | TP_TRANSPORTER: intracellular accumulation in KB-3-1 and MRP1-expressing KB-3-1 cells | 1999 | Molecular pharmacology, May, Volume: 55, Issue:5
| ATP-Dependent efflux of CPT-11 and SN-38 by the multidrug resistance protein (MRP) and its inhibition by PAK-104P. |
AID1386602 | Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay | 2018 | Journal of natural products, 09-28, Volume: 81, Issue:9
| Flabellipparicine, a Flabelliformide-Apparicine-Type Bisindole Alkaloid from Tabernaemontana divaricata. |
AID269202 | Inhibition of human H460 cell growth | 2006 | Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
| Synthesis and cytotoxic activity of polyamine analogues of camptothecin. |
AID249947 | In vitro cytotoxic activity against human HT1197 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1593649 | Cytotoxicity against human TE8 cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives. |
AID624635 | Drug glucuronidation reaction catalyzed by human recombinant UGT1A7 | 2005 | Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
| UDP-glucuronosyltransferases and clinical drug-drug interactions. |
AID249948 | In vitro cytotoxic activity against human U-373MG cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID28876 | Half life for of compound in PBS with RBC suspension | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity. |
AID249921 | In vitro cytotoxic activity against human A-704 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID222931 | Association constant for the binding of lactone form to human serum albumin | 1993 | Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
| Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin. |
AID249931 | In vitro cytotoxic activity against human AL-12T cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1294916 | Cytotoxicity against human HCT15 cells assessed as growth inhibition after 72 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | 10-Boronic acid substituted camptothecin as prodrug of SN-38. |
AID56562 | Cytotoxicity against DNA topoisomerase I purified from calf thymus | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
| Synthesis of water-soluble (aminoalkyl)camptothecin analogues: inhibition of topoisomerase I and antitumor activity. |
AID1194768 | Cytotoxicity against human HT-29 cells after 72 hrs by sulforhodamine B assay | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
| Design, synthesis and biological evaluation of novel homocamptothecin analogues as potent antitumor agents. |
AID679628 | TP_TRANSPORTER: drug resistance(Imatinib mesylate) in BCRP-expressing SaoS2 cells | 2004 | Cancer research, Apr-01, Volume: 64, Issue:7
| Imatinib mesylate is a potent inhibitor of the ABCG2 (BCRP) transporter and reverses resistance to topotecan and SN-38 in vitro. |
AID1470605 | Selectivity ratio of IC50 for human NCI-H460 cells under normoxic condition to IC50 for human NCI-H460 cells under hypoxic condition | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38. |
AID1470602 | Selectivity ratio of IC50 for human HT-29 cells under normoxic condition to IC50 for human HT-29 cells under hypoxic condition | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38. |
AID249954 | In vitro cytotoxic activity against human SK-UT-1B cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID679413 | TP_TRANSPORTER: uptake of SN-38 at a concentration of 0.10uL/oocyte in Xenopus laevis oocytes | 2004 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 32, Issue:3
| Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. |
AID216617 | Relative tumor growth (RTG), calculated by dividing MTW28 by that on day 0 (MTW0) against WiDr xenografts in nude mice at a dose of 10 umol/kg | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
| Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues. |
AID1708540 | Growth inhibition of ARC-111-resistant human HA6n cells by Cell-titer96 assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| Copper(I)-Catalyzed Nitrile-Addition/ |
AID418335 | Antiproliferative activity against human PC6 cells carrying pRC after 6 days | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| Synthesis of new camptothecin analogs with improved antitumor activities. |
AID202842 | Antiproliferative activity against human SKOV-3 ovarian cell line | 1999 | Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17
| BN 80927: a novel homocamptothecin with inhibitory activities on both topoisomerase I and topoisomerase II. |
AID219146 | In Vitro cytotoxicity against human breast cancer cell line (SK-BR-3) | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
| Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues. |
AID1488981 | Selectivity ratio, IC50 for human H460 cells under normoxic condition to IC50 for human H460 cells under hypoxic condition | 2017 | ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
| Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole. |
AID1399559 | Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| A series of camptothecin prodrugs exhibit HDAC inhibition activity. |
AID249941 | In vitro cytotoxic activity against human Panc-1 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID146690 | Cytotoxicity against human non-small-cell lung carcinoma cell line H460 (NSCLC-H460) | 2001 | Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20
| Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity. |
AID216615 | Percentage of inhibition rate (IR) against WiDr xenografts in nude mice at a dose of 10 umol/kg | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
| Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues. |
AID680750 | TP_TRANSPORTER: inhibition of E1S uptake (SN38 10 u M) in OATP1B1-expressing HEK293 cells | 2005 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 33, Issue:3
| Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms. |
AID222926 | % of lactone form at equilibrium in PBS buffer at 37 C in the absence of human serum albumin | 1993 | Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
| Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin. |
AID548079 | Growth inhibition of human lung cancer cells after 72 hrs by sulforhodamine B assay | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
| Synthesis and antitumor activity of novel benzimidazole-5-carboxylic acid derivatives and their transition metal complexes as topoisomerease II inhibitors. |
AID346586 | Induction of human recombinant topoisomerase 1-mediated SV40 DNA cleavage at 1 to 50 uM after 30 mins by PAGE | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Semisynthesis, biological activity, and molecular modeling studies of C-ring-modified camptothecins. |
AID234776 | Tested for (median survival time of treated/control animals) x100 at dosage of 60 mg/kg. | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Antitumor agents. 7. Synthesis and antitumor activity of novel hexacyclic camptothecin analogues. |
AID131159 | Effect in increasing life span of mice bearing L1210 leukemia | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
| Synthesis of water-soluble (aminoalkyl)camptothecin analogues: inhibition of topoisomerase I and antitumor activity. |
AID240049 | Effective concentration against DNA topoisomerase I | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
| Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction. |
AID1222389 | Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Correlation between bilirubin glucuronidation and estradiol-3-gluronidation in the presence of model UDP-glucuronosyltransferase 1A1 substrates/inhibitors. |
AID679172 | TP_TRANSPORTER: drug resistance in BCRP-expressing LLC-PK1 cells | 2003 | Molecular pharmacology, Sep, Volume: 64, Issue:3
| Breast cancer resistance protein exports sulfated estrogens but not free estrogens. |
AID332046 | Cytotoxicity against human H460 cells | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| Synthesis and cytotoxic activity of new 9-substituted camptothecins. |
AID749702 | Inhibition of HDAC8 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Dual-acting histone deacetylase-topoisomerase I inhibitors. |
AID1215100 | Terminal elimination rate constant in cancer patient with severe renal failure administered as infusion after 0.25 to 1.5 hrs by RP-HPLC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Delayed elimination of SN-38 in cancer patients with severe renal failure. |
AID418342 | Ratio of IC50 for human PC6 expressing BCRP cells to IC50 for human PC6 cells carrying pRC | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| Synthesis of new camptothecin analogs with improved antitumor activities. |
AID1535491 | Solubility of the compound in phosphate buffered saline by UV-spectroscopic analysis | 2019 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
| Monodisperse oligoethylene glycols modified Camptothecin, 10-Hydroxycamptothecin and SN38 prodrugs. |
AID1703223 | Induction of apoptosis in human HCT-116 cells assessed as early apoptotic cells level at 0.001 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 0.17%) | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID249917 | In vitro cytotoxic activity against human WiDr cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1428729 | Drug excretion in human urine upto 48 hrs | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
| The long story of camptothecin: From traditional medicine to drugs. |
AID679165 | TP_TRANSPORTER: inhibition of Estrone-3-sulfate uptake(Estrone-3-sulfate: 9.2nM) in Xenopus laevis oocytes | 2005 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 33, Issue:3
| Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms. |
AID133755 | Maximally tolerated dose in mice bearing L1210 leukemia. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
| Synthesis of water-soluble (aminoalkyl)camptothecin analogues: inhibition of topoisomerase I and antitumor activity. |
AID1294919 | Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | 10-Boronic acid substituted camptothecin as prodrug of SN-38. |
AID1593647 | Cytotoxicity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives. |
AID1900082 | Cytotoxicity against human A549 cells assessed as cell growth inhibition incubated for 120 hrs by CCK-8 assay | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
| On-Demand Activation of a Bioorthogonal Prodrug of SN-38 with Fast Reaction Kinetics and High Releasing Efficiency |
AID1708528 | Growth inhibition of human Hep3B cells by Cell-titer96 assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| Copper(I)-Catalyzed Nitrile-Addition/ |
AID680206 | TP_TRANSPORTER: uptake of SN-38 at a concentration of 0.09uL/oocyte in Xenopus laevis oocytes | 2005 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 33, Issue:3
| Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms. |
AID249951 | In vitro cytotoxic activity against human NCI-H727 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1703226 | Induction of apoptosis in human HCT-116 cells assessed as late apoptotic cells level at 1 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 0.07%) | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID245827 | Percent tumor-weight inhibition in mouse tumor sarcoma-180 model after intraperitoneal administration of 5 mg/kg dose in comparison with control mice | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
| Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin. |
AID1708534 | Inhibition of human topoisomerase 1 assessed as stabilization of Topl-DNA cleavable complex by measuring band intensity of free Top-l at 0.1 to 1 uM by band-depletion assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| Copper(I)-Catalyzed Nitrile-Addition/ |
AID249960 | In vitro cytotoxic activity against human MCF7HTB-22 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID249911 | In vitro cytotoxic activity against human FaDu cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1515352 | Antiproliferative activity against human LOXIMVI cells after 48 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
| Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold. |
AID380253 | Inhibition of topoisomerase 1-mediated SV40 DNA cleavage at 1 to 50 uM by gel electrophoresis | 2006 | Journal of natural products, Dec, Volume: 69, Issue:12
| Cucurbitane triterpenes from the fruiting bodies and cultivated mycelia of Leucopaxillus gentianeus. |
AID28494 | % lactone at different intervals of time in human blood. | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity. |
AID1488982 | Selectivity ratio, IC50 for human HT-29 cells under normoxic condition to IC50 for human HT29 cells under hypoxic condition | 2017 | ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
| Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole. |
AID1076086 | Cytotoxicity against human A549 cells | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
| Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs. |
AID247882 | Concentration required to inhibit growth of human cervical HeLa carcinoma cell line | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
| Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction. |
AID83623 | In vitro inhibitory concentration required against HT-29 human colon cancer cells | 2003 | Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5
| Cancer chemotherapy: a SN-38 (7-ethyl-10-hydroxycamptothecin) glucuronide prodrug for treatment by a PMT (Prodrug MonoTherapy) strategy. |
AID1515357 | Antiproliferative activity against human SKOV3 cells after 48 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
| Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold. |
AID91475 | Binding parameter of the carboxylate form to human serum albumin; n value | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
| The structural basis of camptothecin interactions with human serum albumin: impact on drug stability. |
AID1900088 | Dissociation constant pKa of the compound | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
| On-Demand Activation of a Bioorthogonal Prodrug of SN-38 with Fast Reaction Kinetics and High Releasing Efficiency |
AID1561995 | Cytotoxicity agains human HL7702 cells assessed as reduction in cell viability after 72 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
AID249955 | In vitro cytotoxic activity against human SKMEL-28 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1815775 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | 2022 | ACS medicinal chemistry letters, Jan-13, Volume: 13, Issue:1
| The BASHY Platform Enables the Assembly of a Fluorescent Bortezomib-GV1001 Conjugate. |
AID612419 | Stimulation of human recombinant DNA topoisomerase 1-mediated 751-bp BamHI-EcoRV fragment of SV40 DNA cleavage at 1 to 50 uM after 30 mins by polyacrylamide gel-electrophoresis | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
| Synthesis and topoisomerase I inhibitory activity of a novel diazaindeno[2,1-b]phenanthrene analogue of Lamellarin D. |
AID234603 | Tested for (median survival time of treated/control animals) x100 at dosage of 120 mg/kg. | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Antitumor agents. 7. Synthesis and antitumor activity of novel hexacyclic camptothecin analogues. |
AID249923 | In vitro cytotoxic activity against human DLD-1 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID594371 | Cytotoxicity against human HT-29 cells | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Semisynthesis of triptolide analogues: effect of γ-lactone and C-14 substituents on cytotoxic activities. |
AID249933 | In vitro cytotoxic activity against human CAKI-2 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1515359 | Antiproliferative activity against human ACHN cells after 48 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
| Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold. |
AID249950 | In vitro cytotoxic activity against human MALME-3M cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID237674 | Half life of compound for DNA topoisomerase I complex was determined | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
| Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction. |
AID1561993 | Antiproliferative activity against human MIAPaCa2 cells assessed as reduction in cell viability after 72 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
AID222929 | n value for the binding of lactone form to human serum albumin (n value = number of amino acid per binding site) | 1993 | Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
| Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin. |
AID249918 | In vitro cytotoxic activity against human 769-P cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID680548 | TP_TRANSPORTER: uptake of SN-38 at a concentration of 0.16uL/oocyte in Xenopus laevis oocytes | 2005 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 33, Issue:3
| Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms. |
AID1666201 | Cytotoxicity against FR-negative human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging. |
AID1593653 | Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives. |
AID1294921 | Cytotoxicity against human U251 cells assessed as growth inhibition after 72 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | 10-Boronic acid substituted camptothecin as prodrug of SN-38. |
AID1708529 | Growth inhibition of human SJRH30 cells by Cell-titer96 assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| Copper(I)-Catalyzed Nitrile-Addition/ |
AID249940 | In vitro cytotoxic activity against human MES-SA cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID411092 | Cytotoxicity against human A549 cells by SRB method | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
| Semi-synthesis and biological activity of gamma-lactones analogs of camptothecin. |
AID1515344 | Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
| Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold. |
AID1076083 | Cytotoxicity against human HT-29 cells assessed as growth inhibition after 3 days by SRB assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
| Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs. |
AID745328 | Cytotoxicity against human HT-29 cells | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents. |
AID249905 | In vitro cytotoxic activity against human C32 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID244702 | Percent change in body-weight of mouse tumor sarcoma-180 model after intraperitoneal administration of 5 mg/kg dose | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
| Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin. |
AID1541742 | Cytotoxicity against human HeLa cells assessed as cell death at 10 uM after 24 hrs by MTT assay | 2020 | ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
| Mitochondrial Impairment by Cyanine-Based Small Molecules Induces Apoptosis in Cancer Cells. |
AID150520 | In vitro antitumor activity against P388 (murine leukemia) cells. | 1998 | Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
| Synthesis and antitumor activity of ring A- and F-modified hexacyclic camptothecin analogues. |
AID1561994 | Antiproliferative activity against human Capan1 cells assessed as reduction in cell viability after 72 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
AID346585 | Antiproliferative activity against human NCI-H460 cells after short term exposure for 1 hr measured after 72 hrs in drug-free medium | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Semisynthesis, biological activity, and molecular modeling studies of C-ring-modified camptothecins. |
AID223634 | In Vitro cytotoxicity against human ovarian cancer cell line (SK-OV-3) | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
| Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues. |
AID1201344 | Inhibition of human recombinant topoisomerase 1-dependent DNA cleavage using 751-bp BamHI-EcoRI fragment of SV40 DNA at 50 uM incubated for 30 mins by PAGE method | 2015 | European journal of medicinal chemistry, Apr-13, Volume: 94 | Water-soluble isoindolo[2,1-a]quinoxalin-6-imines: in vitro antiproliferative activity and molecular mechanism(s) of action. |
AID249949 | In vitro cytotoxic activity against human ZR-75-1 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID680556 | TP_TRANSPORTER: uptake in OATP1B1-expressing HEK293 cells | 2005 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 33, Issue:3
| Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms. |
AID1222394 | Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation using 4 to 75 uM estradiol by LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Correlation between bilirubin glucuronidation and estradiol-3-gluronidation in the presence of model UDP-glucuronosyltransferase 1A1 substrates/inhibitors. |
AID414758 | Cytotoxicity against human KB3-1 cells after 4 days by MTT method | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
| 12-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridines as novel topoisomerase I-targeting antitumor agents. |
AID221332 | In Vitro cytotoxicity against human lung cancer cell line (A549) | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
| Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues. |
AID216613 | Antitumor activity against MTW28 WiDr xenografts in nude mice at a dose of 10 umol/kg | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
| Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues. |
AID1703222 | Induction of apoptosis in human HCT-116 cells assessed as late apoptotic cells level at 0.001 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 0.07%) | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID1703230 | Solubility of compound in water incubated for 24 hrs under shaking condition by HPLC analysis | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID1222388 | Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Correlation between bilirubin glucuronidation and estradiol-3-gluronidation in the presence of model UDP-glucuronosyltransferase 1A1 substrates/inhibitors. |
AID1488979 | Cytotoxicity against human HT-29 cells assessed as growth reduction under normoxic condition after 72 hrs by MTT assay | 2017 | ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
| Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole. |
AID680984 | TP_TRANSPORTER: inhibition of accumulation by antisense of BCRP in PC-6/SN2-5,PC-6/SN2-5H cells | 2001 | Biochemical and biophysical research communications, Feb-09, Volume: 280, Issue:5
| Breast cancer resistance protein directly confers SN-38 resistance of lung cancer cells. |
AID1562010 | Inhibition of topoisomerase 1 in human A549 cells assessed as increase in phosphorylated KAP1 expression at 0.04 uM after 24 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
AID1703213 | Cytotoxicity against human COLO 205 assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID681563 | TP_TRANSPORTER: Cytotoxicity in MT-4 and MT-4/DOX500 cells | 2003 | Molecular pharmacology, Jan, Volume: 63, Issue:1
| Breast cancer resistance protein (BCRP/ABCG2) induces cellular resistance to HIV-1 nucleoside reverse transcriptase inhibitors. |
AID222924 | % of lactone form at equilibrium in HSA buffer at 37 C in the presence of human serum albumin | 1993 | Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
| Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin. |
AID1900084 | Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
| On-Demand Activation of a Bioorthogonal Prodrug of SN-38 with Fast Reaction Kinetics and High Releasing Efficiency |
AID1515366 | Antiproliferative activity against human DU145 cells after 48 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
| Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold. |
AID1754553 | Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs | 2021 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 46 | New camptothecin derivatives for generalized oncological chemotherapy: Synthesis, stereochemistry and biology. |
AID55802 | Antiproliferative activity against human DU145 prostate cell line | 1999 | Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17
| BN 80927: a novel homocamptothecin with inhibitory activities on both topoisomerase I and topoisomerase II. |
AID1708526 | Growth inhibition of human MDA-MB-231 cells by Cell-titer96 assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| Copper(I)-Catalyzed Nitrile-Addition/ |
AID249908 | In vitro cytotoxic activity against human A427 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1561991 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
AID249914 | In vitro cytotoxic activity against human LoVo cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID248674 | In-vitro inhibitory concentration for human tumor HL60 cell-line was determined using SRB assay after 3 days of incubation | 2005 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
| Synthesis and antitumor activity of the hexacyclic camptothecin derivatives. |
AID331823 | Antiproliferative activity against human H460 cells after 1 hr of drug exposure measured after 72 hrs | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| E-ring-modified 7-oxyiminomethyl camptothecins: Synthesis and preliminary in vitro and in vivo biological evaluation. |
AID242837 | Stability constant for DNA topoisomerase I complex in competitive DNA assay | 2004 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
| Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction. |
AID163143 | Tested in vitro for the inhibition of QG-56 (human lung squamous cell carcinoma) cell line by MTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Antitumor agents. 7. Synthesis and antitumor activity of novel hexacyclic camptothecin analogues. |
AID1561999 | Induction of cell cycle arrest in human A549 cells at 3 to 10 nM after 24 hrs by RNase A/PI-staining based flow cytometric analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
AID253444 | Lethal toxicity against mouse tumor sarcoma-180 model after intraperitoneal administration of 5 mg/kg dose expressed as number of deaths out of 10 mice | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
| Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin. |
AID1666195 | Cytotoxicity against FR-positive human SKHEP1 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging. |
AID249957 | In vitro cytotoxic activity against human MiaPaca-2 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1194769 | Inhibition of topoisomerase 1 (unknown origin) at 100 uM using supercoiled pBR322 DNA substrate by ethidium bromide staining based electrophoresis method | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
| Design, synthesis and biological evaluation of novel homocamptothecin analogues as potent antitumor agents. |
AID1562000 | Induction of cell cycle arrest in human HCT116 cells at 3 nM after 24 hrs by RNase A/PI-staining based flow cytometric analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
AID1703216 | Cytotoxicity against human NCI-H1975 assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID426063 | Antitumor activity against human HT-29 cells by SRB method | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| 7-Cycloalkylcamptothecin derivatives: Preparation and biological evaluation. |
AID1703225 | Induction of apoptosis in human HCT-116 cells assessed as early apoptotic cells level at 0.03 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 0.17%) | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID216614 | Percentage of complete regression (CR) against WiDr xenografts in nude mice at a dose of 10 umol/kg | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
| Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues. |
AID1488977 | Cytotoxicity against human NCI-H460 cells assessed as growth reduction under normoxic condition after 72 hrs by MTT assay | 2017 | ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
| Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole. |
AID249919 | In vitro cytotoxic activity against human 786-O cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1294922 | Inhibition of topoisomerase 1 (unknown origin) assessed as reduction in enzyme-mediated relaxation of supercoiled pBR322 DNA at 100 uM after 30 mins by agarose gel electrophoresis | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | 10-Boronic acid substituted camptothecin as prodrug of SN-38. |
AID91477 | Association constant for the binding of the carboxylate form to human serum albumin;(M aa)e-1 | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
| The structural basis of camptothecin interactions with human serum albumin: impact on drug stability. |
AID1703214 | Cytotoxicity against human Raji assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID1515363 | Antiproliferative activity against human MKN28 cells after 48 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
| Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold. |
AID1708527 | Growth inhibition of human HCT-116 cells by Cell-titer96 assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| Copper(I)-Catalyzed Nitrile-Addition/ |
AID249907 | In vitro cytotoxic activity against human A204 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID234605 | Tested for (median survival time of treated/control animals) x100 at dosage of 240 mg/kg. | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Antitumor agents. 7. Synthesis and antitumor activity of novel hexacyclic camptothecin analogues. |
AID1470603 | Cytotoxicity against human NCI-H460 cells pretreated for 24 hrs under hypoxic condition followed by compound washout measured after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38. |
AID690722 | Cytotoxicity against human A2780 cells overexpressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
| Camptothecins in tumor homing via an RGD sequence mimetic. |
AID745329 | Inhibition of topoisomerase 1 (unknown origin)-mediated DNA cleavage at 1 uM relative to SN-38 | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents. |
AID222928 | n value for the binding of carboxylate form to human serum albumin (n value = number of amino acid per binding site) | 1993 | Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
| Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin. |
AID1561992 | Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by SRB assay | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
AID1708530 | Growth inhibition of human A498 cells by Cell-titer96 assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| Copper(I)-Catalyzed Nitrile-Addition/ |
AID249936 | In vitro cytotoxic activity against human HT1080 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1190166 | Cytotoxicity against drug-resistant human S1-M1-80 cells expressing ABCG2 G482 mutant after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
| IND-2, a pyrimido[1″,2″:1,5]pyrazolo[3,4-b]quinoline derivative, circumvents multi-drug resistance and causes apoptosis in colon cancer cells. |
AID1561987 | Drug uptake in human A549 cells assessed as maximum emission peaks at 430 nm at 5 uM by fluorescence emission spectral analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
AID749704 | Inhibition of HDAC1 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Dual-acting histone deacetylase-topoisomerase I inhibitors. |
AID249953 | In vitro cytotoxic activity against human SK-LMS-1 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID418331 | Antiproliferative activity against human HCT116 cells after 3 days | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| Synthesis of new camptothecin analogs with improved antitumor activities. |
AID248707 | In-vitro inhibitory concentration for human tumor HCT116 cell-line was determined using MTT assay after 3 days of incubation | 2005 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
| Synthesis and antitumor activity of the hexacyclic camptothecin derivatives. |
AID1488980 | Cytotoxicity against human HT-29 cells assessed as growth reduction under hypoxic condition after 72 hrs by MTT assay | 2017 | ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
| Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole. |
AID248760 | In vitro inhibitory concentration against human lung large cell carcinoma cell line, H460 (after 1 hour exposure) | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
| Synthesis and cytotoxic activity of substituted luotonin A derivatives. |
AID211091 | The compound was tested for top1-induced DNA cleavage activity; +++ indicates much more potent than CPT | 1998 | Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
| Molecular modeling studies of the DNA-topoisomerase I ternary cleavable complex with camptothecin. |
AID249965 | In vitro cytotoxic activity against human SW1783 cancer cell lines after 3 days of culture; Activity expressed as log IC50 | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1666197 | Cytotoxicity against FR-positive human SiHa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging. |
AID100463 | Inhibitory activity in mice bearing L1210 leukemia | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
| Synthesis of water-soluble (aminoalkyl)camptothecin analogues: inhibition of topoisomerase I and antitumor activity. |
AID1708523 | Inhibition of human topoisomerase 1 assessed as stabilization of Topl-DNA cleavable complex by measuring DNA cleavage at 50 uM by ethidium bromide dye based agarose gel electrophoresis | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| Copper(I)-Catalyzed Nitrile-Addition/ |
AID1703228 | Solubility of compound in phosphate buffer at pH 4.5 incubated for 24 hrs under shaking condition by HPLC analysis | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID249910 | In vitro cytotoxic activity against human ACHN cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID150683 | Tested in vitro for the inhibition of P388 (mouse leukemia) cell line by MTT assay; 1.95-6.93 ng/mL | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Antitumor agents. 7. Synthesis and antitumor activity of novel hexacyclic camptothecin analogues. |
AID81341 | Tested in vitro for the inhibition of HOC-21(human ovarian cancer) cell line by MTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Antitumor agents. 7. Synthesis and antitumor activity of novel hexacyclic camptothecin analogues. |
AID680207 | TP_TRANSPORTER: uptake of SN-38 at a concentration of 0.09uL/oocyte in Xenopus laevis oocytes | 2004 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 32, Issue:3
| Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. |
AID102138 | Inhibition against MDA-MB-435 S human breast cancer cells in the presence of 30 mg/mL HSA | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity. |
AID321559 | Antiproliferative activity against human MIA PaCa cells after 96 hrs | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Synthesis and bioevaluation of 22-hydroxyacuminatine analogs. |
AID745331 | Cytotoxicity against mouse L1210 cells | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents. |
AID249928 | In vitro cytotoxic activity against human SCC-9 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID249926 | In vitro cytotoxic activity against human Hs 729 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1515332 | Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
| Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold. |
AID1076084 | Cytotoxicity against human HCT116 cells assessed as growth inhibition after 3 days by SRB assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
| Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs. |
AID681562 | TP_TRANSPORTER: uptake in BCRP-expressing PC-6 cells | 2004 | International journal of cancer, Jul-20, Volume: 110, Issue:6
| Novel camptothecin analogues that circumvent ABCG2-associated drug resistance in human tumor cells. |
AID1593652 | Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives. |
AID679164 | TP_TRANSPORTER: uptake in OATP1B1-expressing HEK293 cell | 2004 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 32, Issue:3
| Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. |
AID1754551 | Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs | 2021 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 46 | New camptothecin derivatives for generalized oncological chemotherapy: Synthesis, stereochemistry and biology. |
AID249929 | In vitro cytotoxic activity against human SW948 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID418332 | Antiproliferative activity against human QG56 cells after 3 days | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| Synthesis of new camptothecin analogs with improved antitumor activities. |
AID1703227 | Induction of apoptosis in human HCT-116 cells assessed as early apoptotic cells level at 1 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 0.17%) | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID1535492 | Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
| Monodisperse oligoethylene glycols modified Camptothecin, 10-Hydroxycamptothecin and SN38 prodrugs. |
AID1754552 | Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth measured after 72 hrs | 2021 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 46 | New camptothecin derivatives for generalized oncological chemotherapy: Synthesis, stereochemistry and biology. |
AID1703211 | Cytotoxicity against human HCT-116 assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID1650404 | Antiproliferative activity against human G317 cell spheroid assessed as reduction in cell viability incubated for 8 days | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Pyrazolopyrimide library screening in glioma cells discovers highly potent antiproliferative leads that target the PI3K/mTOR pathway. |
AID249938 | In vitro cytotoxic activity against human Hs 578.T cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID682062 | TP_TRANSPORTER: uptake in membrane vesicle from PC-6/SN2-5H cells | 2001 | Biochemical and biophysical research communications, Nov-09, Volume: 288, Issue:4
| Transport of 7-ethyl-10-hydroxycamptothecin (SN-38) by breast cancer resistance protein ABCG2 in human lung cancer cells. |
AID1626190 | Synergistic cytotoxicity in human HT-29 cells assessed as dose reduction index ratio in presence of CoCl2-induced hypoxic conditions measured at 70 % cell growth inhibition after 72 hrs in presence of compound-5c by cell counter method | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| 1,2-Benzisothiazole Derivatives Bearing 4-, 5-, or 6-Alkyl/arylcarboxamide Moieties Inhibit Carbonic Anhydrase Isoform IX (CAIX) and Cell Proliferation under Hypoxic Conditions. |
AID1593651 | Cytotoxicity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives. |
AID91478 | Association constant for the binding of the lactone form to human serum albumin;(M aa)e-1 | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
| The structural basis of camptothecin interactions with human serum albumin: impact on drug stability. |
AID222930 | Association constant for the binding of carboxylate form to human serum albumin | 1993 | Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
| Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin. |
AID249924 | In vitro cytotoxic activity against human DU145 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID249920 | In vitro cytotoxic activity against human A-498 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID249927 | In vitro cytotoxic activity against human LNCaP cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID28491 | % lactone at different intervals of time in PBS suspension | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity. |
AID1666196 | Cytotoxicity against FR-positive human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
| Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging. |
AID680557 | TP_TRANSPORTER: uptake in OATP1B1-expressing HEK293 cells | 2004 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 32, Issue:3
| Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. |
AID91476 | Binding parameter of the lactone form to human serum albumin; n value | 1994 | Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
| The structural basis of camptothecin interactions with human serum albumin: impact on drug stability. |
AID249966 | In vitro cytotoxic activity against human CFPAC-1 cancer cell lines after 3 days of culture; Activity expressed as log IC50 | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID249959 | In vitro cytotoxic activity against human Detroit 562 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID249909 | In vitro cytotoxic activity against human A549 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1465636 | AUC (0 to t) in Beagle dog at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle. |
AID249964 | In vitro cytotoxic activity against human SW1088 cancer cell lines after 3 days of culture; Activity expressed as log IC50 | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID749697 | Cytotoxicity against human DU145 cells assessed as inhibition of cell viability after 72 hrs by MTS assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Dual-acting histone deacetylase-topoisomerase I inhibitors. |
AID1076088 | Cytotoxicity against human MDA-MB-231 cells | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
| Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs. |
AID1900078 | Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
| On-Demand Activation of a Bioorthogonal Prodrug of SN-38 with Fast Reaction Kinetics and High Releasing Efficiency |
AID411093 | Cytotoxicity against human HT-29 cells by SRB method | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
| Semi-synthesis and biological activity of gamma-lactones analogs of camptothecin. |
AID28883 | Half life of compound in PBS with HSA suspension | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity. |
AID749701 | Inhibition of HDAC in human HeLa cells using Fluor-de-Lys as substrate up to 10 uM after 15 mins by fluorescence assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Dual-acting histone deacetylase-topoisomerase I inhibitors. |
AID331825 | Antiproliferative activity against human HT29 cells after 1 hr of drug exposure measured after 72 hrs | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| E-ring-modified 7-oxyiminomethyl camptothecins: Synthesis and preliminary in vitro and in vivo biological evaluation. |
AID27448 | Half-life period in PBS buffer at 37 C in the absence of human serum albumin | 1993 | Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
| Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin. |
AID211111 | Inhibition of topoisomerase-1 compared to SN-38. | 1998 | Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
| Synthesis and antitumor activity of ring A- and F-modified hexacyclic camptothecin analogues. |
AID249961 | In vitro cytotoxic activity against human H4 cancer cell lines after 3 days of culture; Activity expressed as log IC50 | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1515347 | Antiproliferative activity against human NCI-H522 cells after 48 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
| Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold. |
AID249912 | In vitro cytotoxic activity against human G361 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID249958 | In vitro cytotoxic activity against human MDA-MB-231 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID249934 | In vitro cytotoxic activity against human HCT-15 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID682116 | TP_TRANSPORTER: inhibition of E1S uptake (SN38 10 u M) in OATP1B1-expressing HEK293 cells | 2004 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 32, Issue:3
| Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. |
AID163139 | In vitro antitumor activity against QG-56 (human lung cancer) cells. | 1998 | Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
| Synthesis and antitumor activity of ring A- and F-modified hexacyclic camptothecin analogues. |
AID1294918 | Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | 10-Boronic acid substituted camptothecin as prodrug of SN-38. |
AID249962 | In vitro cytotoxic activity against human Hs 683 cancer cell lines after 3 days of culture; Activity expressed as log IC50 | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1535493 | Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
| Monodisperse oligoethylene glycols modified Camptothecin, 10-Hydroxycamptothecin and SN38 prodrugs. |
AID103441 | Antiproliferative activity against human MCF-7 breast cell line | 1999 | Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17
| BN 80927: a novel homocamptothecin with inhibitory activities on both topoisomerase I and topoisomerase II. |
AID1562006 | Downregulation of TOP1 expression in human A549 cells at 0.04 uM after 24 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
AID1655975 | Cytotoxicity against human RPMI7951 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Artemisinin Derivatives with Antimelanoma Activity Show Inhibitory Effect against Human DNA Topoisomerase 1. |
AID1294920 | Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | 10-Boronic acid substituted camptothecin as prodrug of SN-38. |
AID221333 | In Vitro cytotoxicity against human lung cancer cell line (H128) | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
| Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues. |
AID749695 | Inhibition of HDAC in human DU145 cells assessed as upregulation of p21waf1 expression at 0.1 to 0.5 uM after 24 hrs by Western blot analysis | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Dual-acting histone deacetylase-topoisomerase I inhibitors. |
AID1626188 | Synergistic cytotoxicity in human HT-29 cells assessed as dose reduction index ratio in presence of CoCl2-induced hypoxic conditions measured at 90 % cell growth inhibition after 72 hrs in presence of compound-5c by cell counter method | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| 1,2-Benzisothiazole Derivatives Bearing 4-, 5-, or 6-Alkyl/arylcarboxamide Moieties Inhibit Carbonic Anhydrase Isoform IX (CAIX) and Cell Proliferation under Hypoxic Conditions. |
AID331827 | Resistant index, ratio of IC50 for BCRP overexpressing mitoxantrone-resistant human HT29 cells to IC50 for human HT29 cells | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| E-ring-modified 7-oxyiminomethyl camptothecins: Synthesis and preliminary in vitro and in vivo biological evaluation. |
AID249932 | In vitro cytotoxic activity against human BxPC-3 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1703224 | Induction of apoptosis in human HCT-116 cells assessed as late apoptotic cells level at 0.03 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 0.07%) | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID414760 | Cytotoxicity against BCRP overexpressing human KBH5.0 cells after 4 days by MTT method | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
| 12-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridines as novel topoisomerase I-targeting antitumor agents. |
AID1562011 | Inhibition of topoisomerase 1 in human HCT116 cells assessed as increase in phosphorylated KAP1 expression at 0.04 uM after 24 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
AID1428728 | Mean residence time in human | 2017 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
| The long story of camptothecin: From traditional medicine to drugs. |
AID102137 | Inhibition against MDA-MB-435 S human breast cancer cells in the absence of albumin | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity. |
AID211118 | Average concentration to cause 50% inhibition of topo 1 using the cleavable complex assay | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
| Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues. |
AID1562001 | Induction of cell cycle arrest in human Capan1 cells at 3 nM after 24 hrs by RNase A/PI-staining based flow cytometric analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
AID1470600 | Cytotoxicity against human HT-29 cells pretreated for 24 hrs under hypoxic condition followed by compound washout measured after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38. |
AID1562007 | Downregulation of TOP1 expression in human HCT116 cells at 0.04 uM after 24 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
| Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation. |
AID678799 | TP_TRANSPORTER: increase of cytotoxicity by GF120918 in T8 cells | 2001 | Clinical cancer research : an official journal of the American Association for Cancer Research, Apr, Volume: 7, Issue:4
| Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918. |
AID1703215 | Cytotoxicity against human Hela assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID1708439 | Cytotoxicity against wild-type MDCK-II cells assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Rational drug design of 6-substituted 4-anilino-2-phenylpyrimidines for exploration of novel ABCG2 binding site. |
AID27126 | Equilibrium association constant interacting with unilamellar vesicles of negatively charged DMPG in PBS buffer at pH of 7.4 and 37 degrees celsius. | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity. |
AID624634 | Drug glucuronidation reaction catalyzed by human recombinant UGT1A6 | 2005 | Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
| UDP-glucuronosyltransferases and clinical drug-drug interactions. |
AID1900069 | Solubility of compound in PBS | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
| On-Demand Activation of a Bioorthogonal Prodrug of SN-38 with Fast Reaction Kinetics and High Releasing Efficiency |
AID624637 | Drug glucuronidation reaction catalyzed by human recombinant UGT1A9 | 2005 | Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
| UDP-glucuronosyltransferases and clinical drug-drug interactions. |
AID1593646 | Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives. |
AID1470604 | Cytotoxicity against human NCI-H460 cells pretreated for 24 hrs under normoxic condition followed by compound washout measured after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38. |
AID548078 | Growth inhibition of human gastric cancer cells after 72 hrs by sulforhodamine B assay | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
| Synthesis and antitumor activity of novel benzimidazole-5-carboxylic acid derivatives and their transition metal complexes as topoisomerease II inhibitors. |
AID690587 | Cytotoxicity against human PC3 cells expressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
| Camptothecins in tumor homing via an RGD sequence mimetic. |
AID1076085 | Cytotoxicity against human A549 cells assessed as growth inhibition after 3 days by SRB assay | 2014 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
| Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs. |
AID1399552 | Antiproliferative activity against human A549 cells after 72 hrs by SRB assay | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
| A series of camptothecin prodrugs exhibit HDAC inhibition activity. |
AID248720 | In-vitro inhibitory concentration for human tumor BEL-7402 cell-line was determined using MTT assay after 3 days of incubation | 2005 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
| Synthesis and antitumor activity of the hexacyclic camptothecin derivatives. |
AID249913 | In vitro cytotoxic activity against human HT-29 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1708531 | Growth inhibition of human LNCaP cells by Cell-titer96 assay | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| Copper(I)-Catalyzed Nitrile-Addition/ |
AID17281 | Equilibrium association constant interacting with unilamellar vesicles of electroneutral in PBS buffer at pH 7.4 | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity. |
AID222614 | % of lactone form at equilibrium in human plasma | 1993 | Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
| Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin. |
AID1703221 | Inhibition of colony formation in human HCT-116 cells at 1 nM incubated for 12 days by crystal violet dye based assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID249922 | In vitro cytotoxic activity against human BT-20 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID749698 | Inhibition of topoisomerase-1 (unknown origin) assessed as reduction of pBR322 plasmid DNA relaxation at 50 uM after 30 mins by agarose gel electrophoresis | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Dual-acting histone deacetylase-topoisomerase I inhibitors. |
AID418334 | Antiproliferative activity against human PC6 expressing BCRP cells after 6 days | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| Synthesis of new camptothecin analogs with improved antitumor activities. |
AID244680 | Average tumor weight in mouse tumor sarcoma-180 model after intraperitoneal administration of 5 mg/kg dose | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
| Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin. |
AID1703212 | Cytotoxicity against human LoVo assessed as reduction in cell viability measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID249915 | In vitro cytotoxic activity against human PC-3 cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1465631 | Half life in Beagle dog at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
| Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle. |
AID418336 | Inhibition of human topoisomerase 1 | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| Synthesis of new camptothecin analogs with improved antitumor activities. |
AID1167196 | Intrinsic cytotoxicity against HEK293 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
| Converting potent indeno[1,2-b]indole inhibitors of protein kinase CK2 into selective inhibitors of the breast cancer resistance protein ABCG2. |
AID1703219 | Inhibition of human recombinant topoisomerase I using DNA pBR322 as substrate assessed as relaxed DNA at 100 uM incubated for 30 mins by gel electrophoresis analysis relative to control | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent. |
AID1488978 | Cytotoxicity against human NCI-H460 cells assessed as growth reduction under hypoxic condition after 72 hrs by MTT assay | 2017 | ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
| Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole. |
AID31609 | Percent inhibition of acetylcholinesterase using ATCh1 as a substrate | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
| Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues. |
AID1488967 | Drug level in Pd/C using 1 mg 3C-SN38 assessed as compound formation in presence of H2 after 2 hrs by LC/MS method | 2017 | ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
| Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole. |
AID1708533 | Inhibition of human topoisomerase 1 | 2021 | Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
| Copper(I)-Catalyzed Nitrile-Addition/ |
AID331826 | Antiproliferative activity against BCRP overexpressing mitoxantrone-resistant human HT29 cells after 1 hr of drug exposure measured after 72 hrs | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| E-ring-modified 7-oxyiminomethyl camptothecins: Synthesis and preliminary in vitro and in vivo biological evaluation. |
AID548080 | Growth inhibition of human colon cancer cells after 72 hrs by sulforhodamine B assay | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
| Synthesis and antitumor activity of novel benzimidazole-5-carboxylic acid derivatives and their transition metal complexes as topoisomerease II inhibitors. |
AID1294913 | Retention time in human MCF7 cells at 10'-5 M by HPLC analysis | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | 10-Boronic acid substituted camptothecin as prodrug of SN-38. |
AID680549 | TP_TRANSPORTER: uptake of SN-38 at a concentration of 0.16uL/oocyte in Xenopus laevis oocytes | 2004 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 32, Issue:3
| Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. |
AID247637 | Inhibitory concentration against human Bel-7402 liver cancer cell line | 2005 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
| Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin. |
AID81340 | In vitro antitumor activity against HOC-21 (human ovarian cancer) cells. | 1998 | Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
| Synthesis and antitumor activity of ring A- and F-modified hexacyclic camptothecin analogues. |
AID28881 | Half life in human blood. | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity. |
AID1593648 | Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
| Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives. |
AID1815776 | Cytotoxicity against oleic acid-induced human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | 2022 | ACS medicinal chemistry letters, Jan-13, Volume: 13, Issue:1
| The BASHY Platform Enables the Assembly of a Fluorescent Bortezomib-GV1001 Conjugate. |
AID249944 | In vitro cytotoxic activity against human U87MG cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID679166 | TP_TRANSPORTER: inhibition of Estrone-3-sulfate uptake(Estrone-3-sulfate: 9.2nM) in Xenopus laevis oocytes | 2004 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 32, Issue:3
| Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. |
AID249963 | In vitro cytotoxic activity against human Hs 766.T cancer cell lines after 3 days of culture; Activity expressed as log IC50 | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1182589 | Inhibition of human recombinant topoisomerase 1 at 100 nM preincubated for 20 mins before addition of supercoiled plasmid DNA by ethidium bromide dye based gel electrophoresis | 2014 | Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
| Design, synthesis, mechanisms of action, and toxicity of novel 20(s)-sulfonylamidine derivatives of camptothecin as potent antitumor agents. |
AID219883 | In Vitro cytotoxicity against human colon cancer cell line (WiDr) | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
| Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues. |
AID216616 | Percentage of 50% or greater regression (PR) against WiDr xenografts in nude mice at a dose of 10 umol/kg | 2001 | Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
| Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues. |
AID1194767 | Cytotoxicity against human HCT116 cells after 72 hrs by sulforhodamine B assay | 2015 | Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
| Design, synthesis and biological evaluation of novel homocamptothecin analogues as potent antitumor agents. |
AID28492 | % lactone at different intervals of time in PBS with HSA suspension | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity. |
AID249930 | In vitro cytotoxic activity against human T-47D cancer cell lines after 3 days of culture | 2005 | Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
| Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347169 | Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347414 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347161 | Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347157 | Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |