Hit Identification and Biological Evaluation of Anticancer Pyrazolopyrimidines Endowed with Anti‐inflammatory Activity

Synthesis of Pyrazolo[1,5‐a][1,3,5]triazine, Pyrazolo[1,5‐a]pyrimidine, and Imidazo[1,2‐b]pyrazole Derivatives Based on Imidazo[2,1‐b]thiazole Moiety

“…Also, a literature survey revealed that pyrazolo[1,5‐ a ]pyrimidines are of considerable chemical and pharmacological importance as purine analogs. The class of pyrazolopyrimidines possesses a broad spectrum of biological effectiveness such as antimicrobial , anti‐inflammatory , cytotoxicity , and hepatitis C virus inhibitor activities. Also, imidazo[1,2‐ b ]pyrazole‐type derivatives are an important class of compounds in the medicinal field, with biological applications including anticancer .…”

A facile environment-friendly one-pot two-step regioselective synthetic strategy for 3,7-diarylpyrazolo[1,5-a]pyrimidines related to zaleplon and 3,6-diarylpyrazolo[1,5-a]pyrimidine-7-amines assisted by KHSO $$_{4}$$ 4 in aqueous media

“…Pyrazolopyrimidines have multiple pharmacological activities including anti-inflammatory [1], antitumor [2], antibacterial [3], anti-viral [4], antimetabolites [5], anxiolytic [6], antitrypanosomal [7], antichistosomal [8], and analgesic [9]. They are known to act as CRF 1 antagonist [10].…”

“…It has been found that many pyrazolo[1,5-a]pyrimidine derivatives may block the proliferation of various cancer cell lines [11]. Pyrazolo [1,5-a]pyrimidines are known to be good inhibitors of KDR kinase [12] and COX-2 [1]. Thus, the Electronic supplementary material The online version of this article (doi:10.1007/s11030-015-9606-2) contains supplementary material, which is available to authorized users.…”

“…Thus, the Electronic supplementary material The online version of this article (doi:10.1007/s11030-015-9606-2) contains supplementary material, which is available to authorized users. B Jai Narain Vishwakarma jnvishwakarma@rediffmail.com 1 Organic Research Lab., Department of Chemical Science, Assam Don Bosco University, Airport Road-Azara, Guwahati, Assam 781017, India pyrazolo[1,5-a]pyrimidine scaffold is a novel core structure for estrogen receptor ligands [13]. In addition, sedative agents such as zaleplon and indiplon, as well as the anxiolytic agent ocinaplon, are approved drugs containing a pyrazolo [1,5-a]pyrimidine core ( Fig.…”

Synthesis, Structural Elucidation, and In Vitro Antitumor Activities of Some Pyrazolopyrimidines and Schiff Bases Derived from 5-Amino-3-(arylamino)-1H-pyrazole-4-carboxamides

“…They act as potent inhibitors of the enzymes HCV polymerase [2], checkpoint kinase 1 (CHK1) [3], cyclin-dependent kinase 2 (CDK2) [4], and c-Src kinase [5]. Moreover, pyrazolo[1,5- a ]pyrimidine derivatives have significant antimicrobial [6], antitumor [7], and anti-inflammatory [8] activities.…”