Chromene‐Based Synthetic Chalcones as Potent Antileishmanial Agents: Synthesis and Biological Activity

Abstract

Two types of regioisomeric chromene-based chalcones namely, 1-(6-methoxy-2H-chromen-3-yl)-3-phenylpropen-1-ones and 3-(6-methoxy-2H-chromen-3-yl)-1-phenylpropen-1-ones were prepared and investigated for their antileishmanial activity against promastigotes form of Leishmania major. The obtained results from in vitro biological assays indicated that chloro-substituted 1-(6-methoxy-2H-chromen-3-yl)-3-phenylpropen-1-ones exhibited excellent activity against Leishmania major at non-cytotoxic concentrations.

Induction of apoptosis through tubulin inhibition in human cancer cells by new chromene-based chalcones

“…In our systematic effort to discover novel anticancer agents from synthetic small molecules, a novel class of chromene-based chalcones has been synthesized Foroumadi et al, 2010). These compounds show properties in inhibiting the tumor cell growth.…”

“…Briefly, Claisen-Schmidt condensation of 1-(6-methoxy-2H-chromen-3-yl) ethanone with different aldehydes in ethanol solution of NaOH yielded corresponding chalcones 1-4 Foroumadi et al, 2010). Condensation of 6-methoxy-2H-chromene-3-carbaldehyde or 6-chloro-2H-chromene-3-carbaldehyde with appropriate acetophenone in ethanol solution of NaOH yielded the chalcones 5-16.…”

Crystal structure of 3-amino-8-methoxy-1-(4-methoxy phenyl)-1H-benzo[f]chromene-2-carbonitrile, C22H18N2O3

“…Literature reveals that chromenes and benzochromenes are an important chemical synthon, associated with a broad range of pharmacological activities such as antimicrobial [2][3][4][5], anticancer agent [6] hypolipidemic [7], antioxidant [8,9], analgesic [10], antileishmanial [11,12], vascular-disrupting activity [13], estrogenic anticoagulant and antispasmolytic [14], blood platelet antiaggregating [15] effects and activities. As part of our programmed aim to develop new methodologies for the preparation of 1H-benzo[f ]chromene derivatives [16][17][18], we have synthesized the title compound under microwave irradiation conditions.…”

Ultrasonics Promoted Synthesis of 5-(Pyrazol-4-yl)-4,5-Dihydropyrazoles Derivatives

“…Cyclization of chalcones, leading to pyridine, pyrimidine and pyrazoline derivatives, has been a developing field within the realm of heterocyclic chemistry for the past several years, because of their ready accessibility and the broad spectrum of biological activity of the products [38][39][40][41][42][43][44]. These observations led us to synthesize chalcones and its corresponding pyrazoline, exploring simple procedures.…”