Olga N. Zefirova

Bio: Olga N. Zefirova is an academic researcher from Moscow State University. The author has contributed to research in topics: Adamantane & Tubulin. The author has an hindex of 12, co-authored 105 publications receiving 536 citations. Previous affiliations of Olga N. Zefirova include Russian Academy of Sciences & Russian Academy.

Ligands of the colchicine site of tubulin: A common pharmacophore and new structural classes

Abstract: Structure-activity relationships for ligands of the colchicine site of tubulin were analyzed based on their common pharmacophore. The role of the elucidation of the three-dimensional structure of the colchicine site of tubulin on the development of studies aimed at the search for the ligands of this site is analyzed.

Taxol: Synthesis, bioactive conformations, and structure-activity relationships in its analogs

Abstract: The review describes the syntheses and probable biologically active conformations of taxol, a natural antitumor agent, and systematizes published data on the structure-activity relations in the series of taxol analogs.

Unusual tubulin-clustering ability of specifically c7-modified colchicine analogues

Abstract: Highly cytotoxic C7-modified colchicine analogues, exemplified by tubuloclustin, promote microtubule disassembly followed by the formation of very stable tubulin clusters, both in vitro and in cells. The proposed mechanism of action of tubuloclustin and its analogues, beyond that of colchicine, includes additional specific interactions with the α-tubulin subunit.

Synthesis and study of NOS-inhibiting activity of 2-N-acylamino-5,6-dihydro-4H-1,3-thiazine

Abstract: The synthesis and results of in vitro and in vivo testing of 2-N-acetylamino-, 2-N-benzoylamino-,2-N-cyclohexanecarbonylamino-, and 2-N-(1-adamantanecarbonyl)amino-5,6-dihydro-4H-1,3-thiazines for NOS-inhibiting activity have been described.

If C-H bonds could talk: selective C-H bond oxidation.

Abstract: C-H oxidation has a long history and an ongoing presence in research at the forefront of chemistry and interrelated fields. As such, numerous highly useful articles and reviews have been written on this subject. Logically, these are generally written from the perspective of the scope and limitations of the reagents employed. This Minireview instead attempts to emphasize chemoselectivity imposed by the nature of the substrate. Consequently, many landmark discoveries in the field of C-H oxidation are not discussed, but hopefully the perspective taken herein will allow C-H oxidation reactions to be more readily incorporated into synthetic planning.

Update on melatonin receptors: IUPHAR Review 20.

Abstract: Melatonin receptors are seven transmembrane-spanning proteins belonging to the G protein-coupled receptor super-family. In mammals, two melatonin receptor subtypes exit MT1 and MT2 encoded by the MTNR1A and MTNR1B genes, respectively. The current review provides an update on melatonin receptors by the corresponding sub-committee of the International Union of Basic and Clinical Pharmacology. We will highlight recent developments of melatonin receptor ligands, including radioligands and give an update on the latest phenotyping results of melatonin receptor knockout mice. The current status and perspectives of the structure of melatonin receptor structures will be summarized. The physiological importance of melatonin receptor dimers and biologically important and type 2 diabetes-associated genetic variants of melatonin receptors will be discussed. The role of melatonin receptors in physiology and disease will be further exemplified by its functions in the immune system and the central nervous system. Finally, antioxidant and free radical scavenger properties of melatonin and its relation to melatonin receptors will be critically addressed.

Oxetanes: Recent Advances in Synthesis, Reactivity, and Medicinal Chemistry

Abstract: The four-membered oxetane ring has been increasingly exploited for its contrasting behaviors: its influence on physicochemical properties as a stable motif in medicinal chemistry and its propensity to undergo ring-opening reactions as a synthetic intermediate. These applications have driven numerous studies into the synthesis of new oxetane derivatives. This review takes an overview of the literature for the synthesis of oxetane derivatives, concentrating on advances in the last five years up to the end of 2015. These methods are clustered by strategies for preparation of the ring and further derivatization of preformed oxetane-containing building blocks. Examples of the use of oxetanes in medicinal chemistry are reported, including a collation of oxetane derivatives appearing in recent patents for medicinal chemistry applications. Finally, examples of oxetane derivatives in ring-opening and ring-expansion reactions are described.