TY - JOUR
T1 - Development of 6H-chromeno[3,4-c]pyrido[3′,2′:4,5]thieno[2,3-e]pyridazin-6-ones as Par-4 secretagogues
AU - Frasinyuk, Mykhaylo S.
AU - Bondarenko, Svitlana P.
AU - Sviripa, Vitaliy M.
AU - Burikhanov, Ravshan
AU - Rangnekar, Vivek M.
AU - Liu, Chunming
AU - Watt, David S.
N1 - Publisher Copyright:
© 2015 Elsevier Ltd. All rights reserved.
PY - 2015/5/25
Y1 - 2015/5/25
N2 - Nitrosation and cyclization of 4-(3-aminothieno[2,3-b]pyridine-2-yl)-2H-chromen-2-ones 1 afforded substituted 6H-chromeno[3,4-c]pyrido[3′,2′:4,5]thieno[2,3-e]pyridazin-6-ones 2 that inhibited the intermediary filament protein, vimentin, at low micromolar concentrations. This inhibition promoted the secretion of Prostate Apoptosis Response-4 protein (Par-4), which selectively triggered apoptosis in prostate cancer cells such as CWR22Rv1, LNCaP-derivative C4-2B, PC-3 and its aggressive analog, PC-3 MM2.
AB - Nitrosation and cyclization of 4-(3-aminothieno[2,3-b]pyridine-2-yl)-2H-chromen-2-ones 1 afforded substituted 6H-chromeno[3,4-c]pyrido[3′,2′:4,5]thieno[2,3-e]pyridazin-6-ones 2 that inhibited the intermediary filament protein, vimentin, at low micromolar concentrations. This inhibition promoted the secretion of Prostate Apoptosis Response-4 protein (Par-4), which selectively triggered apoptosis in prostate cancer cells such as CWR22Rv1, LNCaP-derivative C4-2B, PC-3 and its aggressive analog, PC-3 MM2.
KW - Coumarin
KW - Par-4
KW - Prostate Apoptosis Response-4 protein
KW - Prostate cancer
KW - Pyridazine
KW - Vimentin
UR - http://www.scopus.com/inward/record.url?scp=84939979266&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84939979266&partnerID=8YFLogxK
U2 - 10.1016/j.tetlet.2015.01.028
DO - 10.1016/j.tetlet.2015.01.028
M3 - Article
AN - SCOPUS:84939979266
SN - 0040-4039
VL - 56
SP - 3382
EP - 3384
JO - Tetrahedron Letters
JF - Tetrahedron Letters
IS - 23
ER -
