Synthesis and structure-activity relationship study of 2-(substituted benzylidene)-7-(4-fluorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one derivatives as anticancer agents

Synthesis and anticancer activity of novel fused pyrimidine hybrids of myrrhanone C, a bicyclic triterpene of Commiphora mukul gum resin

“…While the methoxy substituents afforded higher yields of benzylidene compounds (11: 86 %; 4: 81 %), the nitro and carboxy substituents gave the products in moderate yields (5: 65 %; 12: 62 %). The benzylidene compounds with an α,β-unsaturated carbonyl functionality, on treatment with guanidine in presence KOH in ethanol at reflux temperature, afforded the pyrimidines hybrids (13)(14)(15)(16)(17)(18)(19)(20)(21)(22) in 60-75 % yield [14][15][16][17]. Also, in this case the high yielding analogues are those containing methoxy groups (22: 76 %; 15: 75 %).…”

A rapid access to novel and diverse 3-oxothiazolo[3,2- $$c$$ c ]pyrimidine-8-carboxylates using multicomponent Mannich cyclisation reactions

“…under similar reaction conditions (entries 18-22, Table 2). Not surprisingly, double Mannich cyclisation products through both primary amine sides were obtained with all bis-amines in good to excellent yields under reflux overnight (entries 18,19,21,22). However, product 4u was obtained by the reaction of 4, 4 -sulfonyldianiline 2u with 1 in moderate yields with a shorter reaction time (entry 20).…”

“…Also, thiazolo[3,2-a]pyrimidines can be considered as another important derivative of thiazolopyrimidines. Both types exhibit a variety of biological properties, such as antitumor and cytotoxic [3], immunomodulatory [4], antimicrobial [5,6], antipsychotic [7], antiinflammatory [8,9,17], calcium antagonist [10], antiviral [11], antiparkinsonian [12], antiarrhythmic [13], antidepressant [14], anticancer [15,18], and analgesic [16] activities ( Fig. 1).…”

<strong>Synthesis and characterization of 2-arylidene derivatives of thiazolopyrimidines with potential biological activity</strong>

“…In particular, thiazolo [3,2-a]pyrimidine derivatives have been the focus of intense research and several members of this class have been reported to possess analgesic, anti-cancer, anti-microbial, anti-inflammatory and anti-hypertensive activities, as well as inotropic activity; other possible applications include their use as antimalarials, HIV reverse transcriptase inhibitors, and therapeutic agents for neurodegenerative diseases [2,7] .…”

“…While DHPMs have emerged as potential backbones of several calcium channel blockers, antihypertensive agents and neuropeptide Y antagonists, thiazolopyrimidines and their analogues have raised considerable interest as purine isosteres [1][2][3][4][5][6] .…”