A mild and efficient one-pot deprotection of THP/MOM/Ac/Ts ethers and concomitant cyclization of chalcone epoxides to 2-hydroxyindanones and 2'-aminochalcones to aza-flavanones using β-Cyclodextrin in water has been developed. β-CD was found to be highly effective in carrying out deprotection and sequel transformations under eco-friendly environment affording moderate to excellent yields (59-99%) at 60 o C in 8-22 min. Water, an eco-friendly reaction medium, has been utilized for the first time in this reaction. The merits of the presented protocol include high yields, catalyst reusability and preclude use of metals and organic solvents. The present method is very much milder but more advanced than those reported earlier.

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in Wiley Online Library (wileyonlinelibrary.com).Two series of novel flavones and flavone-tanaproget conjugates were designed, synthesized, 125 Iradiolabeled, and evaluated for their antiproliferative activity against human cancer cell lines (MCF-7, MDA-MB-231, and HeLa). They exhibited good-to-excellent in vitro antiproliferative activity. For improving the receptor-binding affinity of synthesized compounds, flavone-tanaproget moieties were linked together through alkyl-alkenyl chain spacer, and the butyl chain was substituted at C-3 position of oxa-and aza-flavones to enhance the lypophilicity of the molecule. These compounds are hypothesized to bind with estrogen and progesterone receptors by docking studies, and binding affinities were shown to increase significantly compared with the reference ligands.

Unless otherwise noted, chemicals were purchased from commercial suppliers at the highest purity grade available and were used without further purification. Solvents were distilled by standard methods. Thin layer chromatography was performed on Merck precoated 0.25 mm silica gel plates (60F-254) using UV light as visualizing agent and/or iodine as developing agent. Silica gel (100-200 mesh) was used for column chromatography. Melting points were performed with Ambassador ® and Digital Melting point apparatus (Nutronics), Popular India.IR spectra were recorded on FT-IR spectrometer and expressed as wave numbers (cm -1 ). 1 H and 13 C NMR spectra were recorded on a Brüker Avance (500 MHz & 125 MHz) & Jeol Resonance ECX (400 MHz & 100 MHz) spectrometer. Spectra were referenced internally to the residual proton resonance in CDCl 3 (δ 7.26 ppm), DMSO-d 6 (δ 2.50ppm) or with tetramethylsilane (TMS, δ 0.00 ppm) as the internal standard. Spectra were referenced internally to the residual proton resonance in CDCl 3 (δ 7.26 ppm), DMSO-d 6 (δ 2.50ppm) or with tetramethylsilane (TMS, δ 0.00 ppm) as the internal standard. Spectra were processed using Bruker Topspin ® 3.0.b.8. Chemical shifts (δ) were reported as part per million (ppm) in δ scale downfield from TMS. 13 C NMR spectra were referenced to CDCl 3 (δ 77.23 ppm, the middle peak) and DMSO-d 6 (δ 39.5 ppm, the middle peak). Coupling constants are expressed in Hz. The following abbreviations are used to explain the multiplicities: s = singlet, d = doublet, t = triplet, dt = doublet of triplet, m = multiplet, br = broad. High-resolution mass spectra (HRMS) were obtained on a BrükermicrOTOF™-Q II mass spectrometer (ESIMS). General procedures Synthesis of Starting Material :1. General procedure for synthesis of compounds (1a-1c, 2a-2c, 5, 6, 7a, 7b, 8a-8c, 10).The synthesis followed the literature procedure.

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