165107-97-1Relevant articles and documents
Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities – Part 1
Das, Debasis,Xie, Lingzhi,Wang, Jingbing,Xu, Xin,Zhang, Zonghua,Shi, Jingli,Le, Xiaoyong,Hong, Jian
, p. 591 - 596 (2019/01/04)
Overexpression of EGFR and HER2 are observed in many breast, ovarian, colon and prostate cancers. The second and third generation irreversible EGFR/HER2 dual kinase inhibitors became popular after the approval of Afatinib by FDA to overcome the mutation related problem. To find efficacious drug candidates, a series of novel quinazoline derivatives were designed, synthesized and evaluated as dual EGFR/HER2 tyrosine kinase (TK) inhibitors. Selected twenty four compounds were reported here with significant inhibitory activities against EGFR/HER2 tyrosine kinases. Several compounds showed nanomolar IC50 values. In vitro studies of quinazoline derivatives were done on NCI-H1975, HCC827, A431, MDA MB-453 cell lines. The compounds 1a, 1d and 1v were found more potent compared to standard drug afatinib. In vivo efficacy study of 1d on nude mice NCI-H1975 tumour xenograft model was discussed.
Palladium-Catalyzed Regioselective Direct Cyanation of Acetanilide Derivatives with K4[Fe(CN)6] by C–H Bond Activation
Kianmehr, Ebrahim,Faghih, Nasser,Tanbakouchian, Arezoo,Mahdavi, Mohammad
, p. 4269 - 4274 (2016/09/14)
A practical, versatile, and efficient method for the palladium-catalyzed direct cyanation of readily available acetanilides with K4[Fe(CN)6] as a safe cyanating agent through C–H bond activation with excellent C2 regioselectivity was developed. This finding represents a new strategy for the synthesis of N-(2-cyanoaryl)acetamides, which are important structural motifs in natural products and pharmaceuticals.
HIV INTEGRASE INHIBITORS
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Page/Page column 23, (2010/11/27)
The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.