Synthesis and biological evaluation of novel sulfonamide derivatives of tricyclic thieno[2,3-d]pyrimidin-4(3H)-ones on melanin synthesis in murine B16 cells
作者： Li Fei Nie , Khurshed Bozorov , Chao Niu , Guozheng Huang , Haji Akber Aisa
DOI: 10.1007/S11164-017-3023-3
关键词:
摘要: Phototherapy with psoralens as photosensitizers is the commonly used method for treatment of vitiligo. Considering structure similarity between and thieno[2,3-d]pyrimidinones, a series novel sulfonamide derivatives containing tricyclic thieno[2,3-d]pyrimidinone were synthesized evaluated melanin synthesis in murine B16 cells. All new compounds characterized by 1H NMR, 13C IR HRMS (ESI). Among them, 6 demonstrated excellent activity than positive control (8-methoxylpsoralen, 8-MOP) more 1.5-fold potency. Compound 11w dichloro substitution at meta-positions benzenesulfonyl moiety was most potent one (658.3 ± 8.7%), exhibiting 5.0-fold stronger 8-MOP (130.9 8.6%). The difluoro analog compound 11o increased cells 4.35-fold potency compared to 8-MOP. These may serve lead further drug discoveries
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