| ID Source | ID |
|---|---|
| PubMed CID | 357194 |
| CHEMBL ID | 154189 |
| SCHEMBL ID | 19493073 |
| MeSH ID | M0167039 |
| Synonym |
|---|
| NSC615284 , |
| adozelesin |
| NCI60_004977 |
| D02773 |
| adozelesin (usan/inn) |
| CHEMBL154189 |
| adolezesin |
| SCHEMBL19493073 |
| Q15633945 |
| CS-0024896 |
| HY-106120 |
| n-[2-(3-methyl-7-oxo-5,10-diazatetracyclo[7.4.0.01,12.02,6]trideca-2(6),3,8-triene-10-carbonyl)-1h-indol-5-yl]-1-benzofuran-2-carboxamide |
Adozelesin is a synthetic analog of the antitumor antibiotic, CC-1065, which alkylates N3 of adenine in the minor DNA groove in a sequence-specific manner. It is capable of rapidly inhibiting DNA replication in treated cells through a trans-acting mechanism and preferentially arrests cells in S phase.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Adozelesin is a synthetic analog of the antitumor antibiotic, CC-1065, which alkylates N3 of adenine in the minor DNA groove in a sequence-specific manner. " | ( Mutation spectra induced by adozelesin in the supF gene of human XP-A fibroblasts. Lee, CS; Lee, SY; Pfeifer, GP, 2010) | 2.1 |
| "Adozelesin is an alkylating minor groove DNA binder that is capable of rapidly inhibiting DNA replication in treated cells through a trans-acting mechanism and preferentially arrests cells in S phase. " | ( Induction of DNA damage responses by adozelesin is S phase-specific and dependent on active replication forks. Beerman, TA; Kuo, SR; Liu, JS; Melendy, T, 2003) | 2.03 |
| "Adozelesin is a DNA alkylating agent that exhibits specificity for the motif A/T, A/T and A." | ( The A/T-specific DNA alkylating agent adozelesin inhibits Plasmodium falciparum growth in vitro and protects mice against Plasmodium chabaudi adami infection. Purcell, LA; Spithill, TW; Yanow, SK, 2006) | 1.33 |
| "Adozelesin is a highly potent alkylating agent that undergoes binding in the minor groove of double-stranded DNA (ds-DNA) at A-T-rich sequences followed by covalent bonding with N-3 of adenine in preferred sequences. " | ( Synergistic and additive combinations of several antitumor drugs and other agents with the potent alkylating agent adozelesin. Adams, EG; Bhuyan, BK; Folz, BA; Smith, KS, 1995) | 1.94 |
| "Adozelesin is a highly potent alkylating agent which has entered clinical trials based on its unique mechanisms of action and broad-spectrum antitumor activity in vivo. " | ( Multidrug resistance is a component of V79 cell resistance to the alkylating agent adozelesin. Abraham, I; Adams, EG; Bhuyan, BK; Kelly, RC; Sampson, KE; Smith, KS, 1993) | 1.95 |
| "Adozelesin is a member of a family of extraordinarily cytotoxic DNA damaging agents that bind to the DNA minor groove in a sequence-specific manner and form covalent adducts with adenines. " | ( Inhibition of initiation of simian virus 40 DNA replication in infected BSC-1 cells by the DNA alkylating drug adozelesin. Beerman, TA; Burhans, WC; Cobuzzi, RJ, 1996) | 1.95 |
| "Adozelesin is a potent synthetic analog that was chosen for clinical development because it had a similar preclinical antitumor spectrum, but did not produce deaths similar to CC-1065 at therapeutic doses." | ( Phase I trial of Adozelesin using the treatment schedule of daily x5 every 3 weeks. Baker, LH; Earhart, RH; Flaherty, L; Foster, BJ; Kasunic, DA; LoRusso, PM; Poplin, E; Valdivieso, M; Wozniak, A; Zalupski, M, 1996) | 1.35 |
| "Adozelesin is a synthetic analog of the antitumor antibiotic CC-1065, which alkylates the N3 of adenine in the minor groove in a sequence-selective manner. " | ( Excision repair of adozelesin-N3 adenine adduct by 3-methyladenine-DNA glycosylases and UvrABC nuclease. Ahn, B; Choi, JH; Jin, SG; Lee, CS; Mar, W; O'Connor, TR, 2001) | 2.08 |
| "Adozelesin (U-73975) is an extremely potent cytotoxic agent which causes 90% lethality, after 2 h exposure in vitro, of Chinese hamster ovary and lung (CHO and V79), mouse melanoma (B16), and human ovarian carcinoma (A2780) cells at 0.33, 0.19, 0.2, and 0.025 ng/ml, respectively. " | ( Lethality, DNA alkylation, and cell cycle effects of adozelesin (U-73975) on rodent and human cells. Adams, EG; Bhuyan, BK; McGovren, JP; Petzold, GL; Smith, KS, 1992) | 1.98 |
| "Adozelesin is a derivative of an extremely cytotoxic compound, CC1065. " | ( In vitro evaluation of a novel chemotherapeutic agent, Adozelesin, in gynecologic-cancer cell lines. Averette, H; Donato, D; Hightower, R; Nguyen, HN; Penalver, M; Perras, J; Ramos, R; Sevin, BU, 1992) | 1.97 |
| "Adozelesin (U-73975) is a potent synthetic cyclopropylpyrroloindole (CPI) analog of the cytotoxic DNA-binding antibiotic, CC-1065. " | ( Adozelesin, a selected lead among cyclopropylpyrroloindole analogs of the DNA-binding antibiotic, CC-1065. DeKoning, TF; Gebhard, I; Kelly, RC; Li, LH; McGovren, JP; Warpehoski, MA, 1991) | 3.17 |
Adozelesin treatment of cells was shown to result in the following: induction of p53 protein levels, hyperphosphorylation of replication protein A (RPA), and disruption of the p53-RPA complex.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Adozelesin treatment inhibits SV40 DNA replication at concentrations that produce adducts on just a small fraction of the intracellular population of SV40 DNA molecules." | ( Inhibition of initiation of simian virus 40 DNA replication in infected BSC-1 cells by the DNA alkylating drug adozelesin. Beerman, TA; Burhans, WC; Cobuzzi, RJ, 1996) | 1.23 |
| "Adozelesin treatment of cells was shown to result in the following: induction of p53 protein levels, hyperphosphorylation of replication protein A (RPA), and disruption of the p53-RPA complex (but not disruption of the RPA-cdc2 complex), indicating that adozelesin treatment triggers cellular DNA damage response pathways." | ( Adozelesin triggers DNA damage response pathways and arrests SV40 DNA replication through replication protein A inactivation. Beerman, TA; Kuo, SR; Liu, JS; McHugh, MM; Melendy, T, 2000) | 2.47 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Since most clinical regimens for tumor therapy consist of several drugs, we investigated the antineoplastic action of Ado in combination with 5-aza-2'-deoxycytidine (5-Aza-CdR), a potent inhibitor of DNA methylation or cytosine arabinoside (Ara-C), a potent inhibitor of DNA synthesis." | ( Evaluation of the antineoplastic activity of adozelesin alone and in combination with 5-aza-2'-deoxycytidine and cytosine arabinoside on DLD-1 human colon carcinoma cells. Côté, S; Momparler, RL, 1993) | 0.55 |
Adozelesin has marginal efficacy in the treatment of metastatic breast cancer at the dosage and schedule used in this study. A dosage suppressor screen identified the budding yeast co-chaperone protein Mge1p as a high copy suppressor of the orc2-1-specific lethal effects.
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID96648 | In vitro concentration required to inhibit 50% growth of murine L1210 leukemia cells | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | Stereoelectronic factors influencing the biological activity and DNA interaction of synthetic antitumor agents modeled on CC-1065. |
| AID152675 | In vivo optimum dose given on days 1, 5, and 9 to mice implanted intraperitoneally with P388 leukemia cells | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | Stereoelectronic factors influencing the biological activity and DNA interaction of synthetic antitumor agents modeled on CC-1065. |
| AID25251 | Pseudo-first order rate constant at pH 3 followed spectrophotometrically | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | Stereoelectronic factors influencing the biological activity and DNA interaction of synthetic antitumor agents modeled on CC-1065. |
| AID46324 | Induced circular dichroism (ICD), expressed as molar ellipticity, in the presence of calf-thymus DNA | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | Stereoelectronic factors influencing the biological activity and DNA interaction of synthetic antitumor agents modeled on CC-1065. |
| AID20503 | Lipophilic/hydrophilic partitioning (RP-TLC) | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | Stereoelectronic factors influencing the biological activity and DNA interaction of synthetic antitumor agents modeled on CC-1065. |
| AID153429 | In vivo % increase in life span of treated animals (OD) over that of control mice bearing tumor, determined against P388 leukemia cells | 1988 | Journal of medicinal chemistry, Mar, Volume: 31, Issue:3 | Stereoelectronic factors influencing the biological activity and DNA interaction of synthetic antitumor agents modeled on CC-1065. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 2 (3.45) | 18.7374 |
| 1990's | 35 (60.34) | 18.2507 |
| 2000's | 18 (31.03) | 29.6817 |
| 2010's | 3 (5.17) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (20.96) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 5 (8.62%) | 5.53% |
| Reviews | 3 (5.17%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 50 (86.21%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||