Synthesis and Cytotoxic Activity of New Flavopiridol Analogs

Abstract

Structural analogs of flavopiridol {2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methyl-4-piperidinyl]-4-chromenone} are attractive as potential antitumor drugs [1]. They can be represented as a chrysine flavonoid in which the C22 H is replaced by Cl; the C8 H, by a N-containing heterocycle (3-hydroxy-N-methylpiperidine in the case of flavopiridol). However, known methods for synthesizing flavopiridol analogs [2, 3] are complicated and multi-step. Therefore, the successful electrochemical synthesis of biflavonoids and their N-containing analogs [4,5] allowed us to propose that it can be used to synthesize new flavopiridol analogs.Chrysine (0.254 g, 1 mmol, Aldrich) was dissolved in MeCN (250 mL), treated with LiClO 4 (0.110 g) and morpholine (0.520 mL), and electrolyzed in a diaphragm cell at a Pt anode with a working surface of 2 cm 2 and current 12 mA. KCl (0.5 g) was mixed with the anode liquor after 3 h of electrolysis, which then was continued for 2.5 h. When the electrolysis was finished, about 90% of the solvent was distilled from the anode liquor. Two red pure compounds were isolated from the residual by column chromatography (Porokvarts PKN-200, CHCl 3 -EtOH, 80:20 v/v, 5 mL/min).The yields of 1 and 2 calculated for starting chrysine were (0.17 ± 0.01 g, 45.2 ± 1.5%) and (0.13 ± 0.01 g, 34.6 ± 1.5%), respectively. 5,7-Dihydroxy-8-morpholino-2-(2-chlorophenyl)-4H-chromen-4-one (1). C 19 H 16 NO 5 Cl, mp 241 r 3qÑ, [D] D 20 +52.7q (c 0.35, MeOH). UV spectrum (MeOH, O max , nm): 210, 305, 346. IR spectrum (KBr, Q max , cm -1 ): 3615, 3340

Effect of combined compression‐vibration therapy using non‐invasive Beautylizer Therapy Cosmospheres V on the subcutaneous tissue morphology in women with gynoid lipodystrophy (pilot study)

“…Applying a non‐invasive Beautylizer Therapy Cosmoshperes V medical device on the skin of women with GLD intensifies microcirculation in the exponential zone, activates lipolysis, and reduces tissue hypoxia manifestations 27–30 …”

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New Approaches to the Surgical Treatment of Lung and Bronchial Tumors in Children

“…In particular, the method of precision resection is used, if possible, which is extremely organpreserving, since the targeted tumor removal is performed while preserving the surrounding tissue. Over the past decades, in addition to mechanical methods, modern hightemperature methods have been used in surgical practice to combine the stage of tissue dissection and arrest of bleeding, followed by their direct welding [1][2].…”

Bending of an Elastic Three-Layer Plate With a Hole Connected to the Soil Foundation

“…and radiation impacts on a sandwich circular plate were considered. The papers [14][15] are devoted to the study of the strength of polymer composite panels with internal defects under the action of an unsteady loading. In the present paper the authors consider the bending of an elastic circular three-layer plate with a central hole connected to the Winkler base.…”