Kyung-Hoon Min

A small molecule accelerates neuronal differentiation in the adult rat.

Adult neurogenesis occurs in mammals and provides a mechanism for continuous neural plasticity in the brain. However, little is known about the molecular mechanisms regulating hippocampal neural progenitor cells (NPCs) and whether their fate can be pharmacologically modulated to improve neural plasticity and regeneration. Here, we report the characterization of a small molecule (KHS101) that selectively induces a neuronal differentiation phenotype. Mechanism of action studies revealed a link of KHS101 to cell cycle exit and specific binding to the TACC3 protein, whose knockdown in NPCs recapitulates the KHS101-induced phenotype. Upon systemic administration, KHS101 distributed to the brain and resulted in a significant increase in neuronal differentiation in vivo. Our findings indicate that KHS101 accelerates neuronal differentiation by interaction with TACC3 and may provide a basis for pharmacological intervention directed at endogenous NPCs.

Asymmetric Total Synthesis of Fluvirucinine A1

Diastereoselective vinyl addition to an amide carbonyl group and amide enolate induced aza-Claisen rearrangement are the key steps in the first asymmetric total synthesis of fluvirucinine A(1) (1), the aglycon of fluvirucin A(1). Fluvirucins are a class of macrolactam antibiotics produced by actinomycete strains that show promising biological properties.

Pimarane cyclooxygenase 2 (COX-2) inhibitor and its structure-activity relationship.

The structure-activity relationship and molecular modelings of a novel pimarane COX-2 inhibitor are reported. Particularly, a series of linker extended analogues designed on the basis of these studies exhibited significantly enhanced COX-2 inhibitory activities and selectivities.

The highly diastereoselective palladium-catalyzed cyclizations. stereoselective syntheses of cis and trans-disubstituted hydroxycyclopentanes

Abstract A new variant of palladium-catalyzed stereoselective cyclization has been developed. This process provides an excellent 1,2-diastereocontrol of two new stereogenic centers as well as 1,3-asymmetric induction. In addition, desulfonylation of the cyclization product with retention of the initial stereochemistry and conversion of the desulfonylation product to the advanced carbaprostacyclin intermediate is described.

A versatile asymmetric synthesis of highly enantiomerically enriched 12(s)-HETE via a combination of enzymatic and chemical processes

This paper describes a versatile asymmetric synthesis of highly enantiomerically enriched 12(S)-HETE via enzymatic kinetic resolution of the key allylic alcohol synthon and the facile introduction of three alkyne units which were concomitantly converted to three alkenes units.

Asymmetrische Totalsynthese von Fluvirucinin A1

Die diastereoselektive Vinyladdition an eine Amid-Carbonylgruppe und die Amidenolat-induzierte Aza-Claisen-Umlagerung sind die Schlusselreaktionen der ersten asymmetrischen Totalsynthese von Fluvirucinin A11, dem Aglycon von Fluvirucin A1. Die von Actinomyceten produzierten Fluvirucine sind Makrolactam-Antibiotika mit interessanten biologischen Eigenschaften.

Facile construction of the oxaphenalene skeleton by peri ring closure. Formal synthesis of mansonone F

A concise and divergent total synthesis of mansonone F has been accomplished via an efficient construction of the oxaphenalene skeleton by facile peri ring closure of the naphthol ether, and an effective preparation of the cyclization precursor starting from readily available 5-methoxy-1-tetralone by employing a palladium-induced aromatization of the naphthalinol.

Synthesis of C4-modified acanthoic acid analogs and their biological evaluation as nitric oxide inhibitors

Synthesis and biological evaluation of a series of C4-modified acanthoic acid analogs are reported. Among them, the analog 7 and 10 exhibit potent cellular inhibitory activity in NO inhibition assay.