BIOE 402. Medical Technology Assessment. 2 or 3 hours. Bioentrepreneur course. Assessment of medical technology in the context of commercialization. Objectives, competition, market share, funding, pricing, manufacturing, growth, and intellectual property; many issues unique to biomedical products. Course Information: 2 undergraduate hours. 3 graduate hours. Prerequisite(s): Junior standing or above and consent of the instructor.

“Bioinformatics” 특집을 내면서

Hybrid molecules: The privileged scaffolds for various pharmaceuticals

Organotin polymers as anticancer and antiviral agents

Histone deacetylase 8 (HDAC8), a unique class I zinc-dependent HDAC, is an emerging target in cancer and other diseases. Its substrate repertoire extends beyond histones to many nonhistone proteins. Besides being a deacetylase, HDAC8 also mediates signaling via scaffolding functions. Aberrant expression or deregulated interactions with transcription factors are critical in HDAC8-dependent cancers. Many potent HDAC8-selective inhibitors with cellular activity and anticancer effects have been reported. We present HDAC8 as a druggable target and discuss inhibitors of different chemical scaffolds with cellular effects. Furthermore, we review HDAC8 activators that revert activity of mutant enzymes. Isotype-selective HDAC8 targeting in patients with HDAC8-relevant cancers is challenging, however, is promising to avoid adverse side effects as observed with pan-HDAC inhibitors.

https://www.future-science.com/doi/pdf/10.4155/fmc-2016-0117

Targeting histone deacetylase 8 as a therapeutic approach to cancer and neurodegenerative diseases.

1,2,3-triazole tethered Indole-3-glyoxamide derivatives as multiple inhibitors of 5-LOX, COX-2 & tubulin: Their anti-proliferative & anti-inflammatory activity.

Synthesis of amino acid appended indoles: appreciable anti-fungal activity and inhibition of ergosterol biosynthesis as their probable mode of action.

Lead modification: amino acid appended indoles as highly effective 5-LOX inhibitors.

N-1, C-3 substituted indoles as 5-LOX inhibitors--in vitro enzyme immunoaasay, mass spectral and molecular docking investigations.

Three new triphenyltin(IV) complexes, viz., triphenylstannyl 2-((E)-(4-hydroxy-3-((E)-((4-(methoxycarbonyl)phenyl)imino)methyl)phenyl)-diazenyl)benzoate (Ph3SnL2H: 2), methyl 2-((E)-(4-hydroxy-3-((E)-((4-(((triphenylstannyl)oxy)carbonyl)phenyl)imino)methyl)phenyl)diazenyl)benzoate (Ph3SnL3H: 3), and triphenylstannyl 2-((E)-(4-hydroxy-3-((E)-((4-(((triphenylstannyl)oxy)carbonyl)phenyl)imino)methyl)phenyl)diazenyl)benzoate ((Ph3Sn)2L4H: 4) were synthesized and characterized by spectroscopic (1H, 119Sn NMR and IR) techniques in combination withelemental analysis. The 119Sn NMR spectral data were recorded in a non-coordinating solvent and indicate tetrahedral coordinationgeometry in solution. In the solid state, a single-crystal X-ray diffraction analysis of the dinuclear complex(Ph3Sn)2L4H (4) revealed a monocapped tetrahedral coordination geometry with anisobidentate coordination modes of thecarboxylate groups with average bond angles around the Sn atoms of 113.5 and 112.2°, respectively. In vitro cytotoxicitystudies were performed with all three complexes 2-4, along with a previously reported parent aquatriphenylstannyl complex,2-((3-formyl-4-hydroxyphenyl)diazenyl)benzoate (Ph3SnL1H.OH2 (1)) across a panel of human tumor cell lines, viz.,A498, EVSA-T, H226, IGROV, M19 MEL, MCF-7 and WIDR. The screening results were compared with those from relatedtriphenyltin(IV) carboxylates containing (i) imino (11-16) and (ii) diazenyl frameworks (1, 5-10). In general, complexes2-4 exhibited good cytotoxic activity and among them, compound 4 was found to be the best performer, particularlyfor EVSA-T and MCF-7 cell lines. Additionally, 4 scored better activity than cisplatin (2-15 folds), 5-fluorouraciland etoposide across a panel of cell lines. Docking studies indicated that the diazenyl and imino nitrogen atoms, and theoxygen atoms of triphenyltin ester, methyl ester and phenolic group play an important role for the complexation of the organotincompounds in the active sites of enzymes such as ribonucleotide reductase (pdb ID: 4R1R), thymidylate synthase(pdb ID: 2G8D), thymidylate phosphorylase (pdb ID: 1BRW) and topoisomerase II (pdb ID: 1QZR).

Advancement Towards Tin-based Anticancer Chemotherapeutics: Structural Modification and Computer Modeling Approach to Drug-Enzyme Interactions

Corrigendum to “Synthesis and evaluation of indole-based new scaffolds for antimicrobial activities—Identification of promising candidates” [Bioorg. Med. Chem. Lett. 21 (2011) 3367–3372]

Pooja

Papers

Synthesis of amino acid appended indoles: appreciable anti-fungal activity and inhibition of ergosterol biosynthesis as their probable mode of action.

Lead modification: amino acid appended indoles as highly effective 5-LOX inhibitors.

N-1, C-3 substituted indoles as 5-LOX inhibitors--in vitro enzyme immunoaasay, mass spectral and molecular docking investigations.

Advancement Towards Tin-based Anticancer Chemotherapeutics: Structural Modification and Computer Modeling Approach to Drug-Enzyme Interactions

Corrigendum to “Synthesis and evaluation of indole-based new scaffolds for antimicrobial activities—Identification of promising candidates” [Bioorg. Med. Chem. Lett. 21 (2011) 3367–3372]