Plant antitumor agents. 18. Synthesis and biological activity of camptothecin analogs was written by Wani, Mansukh C.;Ronman, Peter E.;Lindley, James T.;Wall, Monroe E.. And the article was included in Journal of Medicinal Chemistry in 1980.COA of Formula: C10H10N2O3 The following contents are mentioned in the article:
10-Methoxy, I (R = OMe); 1-aza-, benz[j]- and 18-methoxycamptothecin were obtained by total synthesis from II via III. The 2 water-soluble analogs, I (R = OCH2CO2H, OCH2CH2NEt2) with intact ring E were prepared from natural I (R = OH). In general, there was a good correlation between in vitro 9KB cytotoxicity and activity in the P388 leukemia system. While the aza analog was active in P388 only at a much higher dose level than natural camptothecin (I, R = H), the 18-methoxy analog exhibited activity comparable to that of I (R = H). The water-soluble derivative I (R = OCH2CO2H) was inactive. I (R = OCH2CH2NEt2).HCl showed excellent activity at a high dose level. This could be due to its hydrolysis to I (R = OH), (卤)-camptothecin was roughly half as active as I (R = H) indicating that the isomer is inactive. This study involved multiple reactions and reactants, such as Ethyl 5-cyano-4-methyl-6-oxo-1,6-dihydropyridine-2-carboxylate (cas: 58610-61-0COA of Formula: C10H10N2O3).
Ethyl 5-cyano-4-methyl-6-oxo-1,6-dihydropyridine-2-carboxylate (cas: 58610-61-0) belongs to pyridine derivatives. In contrast to benzene, Pyridine’s electron density is not evenly distributed over the ring, reflecting the negative inductive effect of the nitrogen atom. Pyridine derivatives are also useful as small-molecule 伪-helix mimetics that inhibit protein-protein interactions, as well as functionally selective GABA ligands.COA of Formula: C10H10N2O3