brostallicin: alkylates DNA in the presence of cellular thiols; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 6918408 |
| CHEMBL ID | 1189025 |
| SCHEMBL ID | 3678233 |
| MeSH ID | M0425375 |
| Synonym |
|---|
| pnu-166196a |
| 4-[[4-[[4-[[4-(2-bromoprop-2-enoylamino)-1-methylpyrrole-2-carbonyl]amino]-1-methylpyrrole-2-carbonyl]amino]-1-methylpyrrole-2-carbonyl]amino]-n-[2-(diaminomethylideneamino)ethyl]-1-methylpyrrole-2-carboxamide |
| brostallicin |
| 4-(2-bromoacrylamido)-n'''-(2-guanidinoethyl)-1,1',1',1'''-tetramethyl-n,4':n',4':n',4'''-quater(pyrrole-2-carboxamide) |
| 203258-60-0 |
| rpc6r41k4i , |
| pnu166196 |
| unii-rpc6r41k4i |
| brostallicin [inn] |
| CHEMBL1189025 |
| SCHEMBL3678233 |
| n-(5-(((5-(((2-((aminoiminomethyl)amino)ethyl)amino)carbonyl)-1-methyl-1h-pyrrol-3-yl)amino)carbonyl)-1-methyl-1h-pyrrol-3-yl)-4-(((4-((2-bromo-1-oxo-2-propen-1-yl)amino)-1-methyl-1h-pyrrol-2-yl)carbonyl)amino)-1-methyl-1h-pyrrole-2-carboxamide |
| brostallicin [mi] |
| brostallicin [mart.] |
| 4-(2-bromoacrylamido)-n'''-(2-guanidinoethyl)-1,1',1'',1'''-tetramethyl-n,4':n',4'':n'',4'''-quater(pyrrole-2-carboxamide) |
| brostallicin [who-dd] |
| DTXSID70174222 |
| Q4975412 |
| DB06598 |
| 4-(2-bromoacrylamido)-n-(5-((5-((5-((2-guanidinoethyl)carbamoyl)-1-methyl-1h-pyrrol-3-yl)carbamoyl)-1-methyl-1h-pyrrol-3-yl)carbamoyl)-1-methyl-1h-pyrrol-3-yl)-1-methyl-1h-pyrrole-2-carboxamide |
| 1h-pyrrole-2-carboxamide,n-[5-[[[5-[[[2-[(aminoiminomethyl)amino]ethyl]amino]carbonyl]-1-methyl-1h-pyrrol-3-yl]amino]carbonyl]-1-methyl-1h-pyrrol-3-yl]-4-[[[4-[(2-bromo-1-oxo-2-propenyl)amino]-1-methyl-1h-pyrrol-2-yl]carbonyl]amino]-1-methyl- |
Brostallicin is a DNA minor groove binder that shows enhanced antitumor activity in cells with high glutathione S-transferase (GST)/glutathione content. Brostallicin has shown activity in patients with soft tissue sarcoma (STS) failing first-line therapy.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Brostallicin has a peculiar mechanism of action involving activation upon binding to glutathione (GSH) catalyzed by glutathione-S-transferase (GST)." | ( Brostallicin: a new concept in minor groove DNA binder development. Broggini, M; Fontana, E; Fowst, C; Geroni, C; Marchini, S; Moneta, D, 2004) | 2.49 |
The clearance and terminal half-life of Brostallicin were dose-independent. Blood samples were obtained before and after the first and last infusions during cycle 1.
The precise molecular mechanism of interaction between brostallicin and the other tested cytotoxics has not yet been identified. A clear therapeutic gain is observed in preclinical models when bro stallicin is combined with anticancer agents such as cDDP, DX, CPT-11, and Taxotere.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Although the precise molecular mechanism of interaction between brostallicin and the other tested cytotoxics has not yet been identified, a clear therapeutic gain is observed in preclinical models when brostallicin is combined with anticancer agents such as cDDP, DX, CPT-11, and Taxotere." | ( Enhancement of in vivo antitumor activity of classical anticancer agents by combination with the new, glutathione-interacting DNA minor groove-binder, brostallicin. Broggini, M; Colombo, T; Geroni, C; Marchini, S; Sabatino, MA, 2003) | 0.76 |
| "Escalating doses of brostallicin were administered in combination with a fixed dose of cisplatin (75 mg/m(2)) in patients with recurrent or metastatic advanced solid tumors who had previously received a cumulative dose of cisplatin not higher than 475 mg/m(2)." | ( Phase I dose-escalation study of brostallicin, a minor groove binder, in combination with cisplatin in patients with advanced solid tumors. Airoldi, M; Barone, C; Caponigro, F; Comis, S; Crippa, S; Fiorentini, F; Fornari, G; Jannuzzo, MG; Lorusso, D; MacArthur, R; Merlano, M; Petroccione, A; Schena, M; Weitman, S, 2010) | 0.97 |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 13 (76.47) | 29.6817 |
| 2010's | 4 (23.53) | 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 (18.76) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 5 (29.41%) | 5.53% |
| Reviews | 2 (11.76%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 10 (58.82%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||