Phospholipase C Inhibitors: A New Class of Agents

Abstract

A series of nitrocoumarin and nitrochromene derivatives have been prepared and shown to inhibit the phosphatidylinositol-specific phospholipase C(PLC)(IC50 < 10 micrograms/mL) isolated from human melanoma. The inhibition of PLC by nitrocoumarin 4a was time-dependent and irreversible. The inhibition of PLC was shown to interfere with inositide metabolism in whole cells (IC50 = 4 micrograms/mL) in a manner consistent with their proposed mode of activity. Finally, the compounds were shown to be growth inhibitory to cultured melanoma cells (ID50 = 2 micrograms/mL), suggesting that PLC may be an attractive new target for chemotherapeutic intervention.

Ag3[PMo12O40]: An efficient and green catalyst for the synthesis of highly functionalized pyran‐annulated heterocycles via multicomponent reaction

“…Coumarin‐fused pyran‐annulated 4 H ‐chromenes, particularly dihydropyrano[3,2‐ c ]chromene and chromeno[4,3‐ b ]chromene derivatives, have attracted much attention of synthetic organic and medicinal chemists due to their exhibiting various biological properties as such as antitumour, anticancer, antimalaria, anti‐Alzheimer, anti‐HIV, antibacterial, anticoagulant and anti‐anaphylactic activities. A selection of such biologically potent molecules is depicted in Figure .…”

Sustainable and Eco‐Friendly Method for the Synthesis of Some Bioactive Derivatives of Biscoumarin and Pyrano[3,2‐c]Chromene‐3‐Carbonitrile Using Taurine, as the Catalyst

“…Recently, pyrano[3,2‐ c ]chromene‐3‐carbonitriles and their derivatives have been under attentions because of their vast range of chemical and biological properties such as spasmolytic, diuretic, anticancer, anticoagulant, antianaphylactic,, cytotoxic, antitumor, antimicrobial and antituberculosis activities ,. Also, they have been used as treatments for neuro‐destructing diseases including Huntington, Parkinson, Alzheimer, also as a remedy for the treatment of Myoclonus and Schizophrenia, ischemic behavior and Dawn's syndrome …”

Microwave Assisted One Pot Synthesis of 3,4-Dihydropyrano[c]chromene Derivatives using [Emim]OH Ionic Liquid as Novel Catalyst

“…Chromene derivatives are structural moiety commonly found in most of the alkaloids with manifesting diverse biological activities [3,4]. The dihydropyrano[c]chromenes derivatives has fascinated attention of an important class of heterocyclic chemistry having useful pharmacological and biological activity such as analgesic [5], anti-HIV [6], anticancer [7], antituberculosis agents [8], anticoagulant [9], antibacterial [10], anti-Alzheimer [11], antimalarial [5], antimicrobials [8], antifungal [12], molluscidal [13], acetyl cholinesterase inhibitor [14] and anti-inflammatory [15]. The derivatives of dihydropyrano [2,3-c]chromene can also be employed as cosmetic pigment and utilized as potential biodegradable agrochemical [16].…”