1595286-21-7Relevant articles and documents
6-Cinnamoyl-4-arylaminothienopyrimidines as highly potent cytotoxic agents: Design, synthesis and structure-activity relationship studies
Aghcheli, Ayoub,Bakhshaiesh, Tayebeh Oghabi,Esmaeili, Rezvan,Foroumadi, Alireza,Hasanvand, Zaman,Khalaj, Ali,Moghimi, Setareh,Nazeri, Elahe,Salarinejad, Somayeh,Toolabi, Mahsa
, (2020)
In this paper, we described the synthesis and cytotoxic activities of two new series of thieno[2,3-d]pyrimidine and thieno[3,2-d] pyrimidine derivatives. Most of the synthesized compounds had significant antiproliferative activities against PC3, MDA-MB-23
Design, synthesis and biological evaluation of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel histone deacetylase inhibitors
Yang, Wei,Li, Lixuan,Ji, Xun,Wu, Xiaowei,Su, Mingbo,Sheng, Li,Zang, Yi,Li, Jia,Liu, Hong
, p. 6146 - 6155 (2015/02/02)
A series of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel HDACs inhibitors were designed, synthesized and evaluated. Most of these compounds displayed good to excellent inhibitory activities against HDAC1, 3, 6. The IC50 values of compound 10r against HDAC1, HDAC3, HDAC6 was 1.14 ± 0.03 nM, 3.56 ± 0.08 nM, 11.43 ± 0.12 nM. Compound 10r noticeably up-regulated the level of histone H3 acetylation compared to the SAHA. Most of the compounds showed the strong anti-proliferative activity against human cancer cell lines including RMPI8226 and HCT-116. The IC50 values of Compounds 10r and 10t against RPMI8226 was 2.39 ± 0.20 μM, 1.41 ± 0.44 μM, respectively, and the HCT-116 was sensitive to the compounds 10h, 10m, 10r, 10w with the IC50 values 1.9 μM.