Synthesis and Evaluation of a Monomethyl Auristatin E─Integrin αβ Binding Peptide-Drug Conjugate for Tumor Targeted Drug Delivery.

Many anticancer drugs exhibit high systemic off-target toxicities causing severe side effects. Peptide-drug conjugates (PDCs) that target tumor-specific receptors such as integrin αβ are emerging as powerful tools to overcome these challenges. The development of an integrin αβ-selective PDC was achieved by combining the therapeutic efficacy of the cytotoxic drug monomethyl auristatin E with the selectivity of the αβ-binding peptide (αβ-BP) and with the ability of positron emission tomography (PET) imaging by copper-64.

Ultrasensitive colorimetric detection of fluoride and arsenate in water and mammalian cells using recyclable metal oxacalixarene probe: a lateral flow assay.

Globally 3 billion people are consuming water with moderately high concentrations of fluoride and arsenic. The development of a simple point of care (PoC) device or home device for the detection of fluoride/arsenic ensures safety before consuming water. Till date, lateral flow assay (LFA) based PoC devices can detect nucleic acids, viruses and diseases.

TSP-1 (Thrombospondin-1) Deficiency Protects ApoE Mice Against Leptin-Induced Atherosclerosis.

Objective: Hyperleptinemia, hallmark of obesity, is a putative pathophysiologic trigger for atherosclerosis. We previously reported a stimulatory effect of leptin on TSP-1 (thrombospondin-1) expression, a proatherogenic matricellular protein implicated in atherogenesis. However, a causal role of TSP-1 in leptin-driven atherosclerosis remains unknown.

Comparative Study for the Cobalt(II)- and Iron(II)-Mediated Desulfurization of Disulfides Demonstrating That the C-S Bond Cleavage Step Precedes the S-S Bond Cleavage Step.

A unique Co(II)- and Fe(II)-mediated complete desulfurization of disulfides of the type RS-SR and RC(O)S-SC(O)R to yield the corresponding alcohols (ROH) and carboxylic acids (RCOOH), respectively, along with the formation of a dicobalt(II)/diiron(II)-hydrosulfide complex, [M(PhBIMP)(-SH)(DMF)] (M = Co, Fe), has been demonstrated. This new desulfurization reaction involves cleavage of both C-S and S-S bonds, where the cleavage of the S-S bond (presumably two-electron reduction of the S-S bond) may generate two-electron-oxidized dicobalt(III)/diiron(III) species, [M(PhBIMP)(HO)(DMF)] (M = Co, Fe), in solution. While the generation of such a solvent- and/or HO-coordinated dicobalt(III) species in the reaction solution could not be established beyond a doubt, formation of the diiron(III) species [Fe(PhBIMP)(HO)(DMF)] according to the proposed reaction mechanism has been confirmed by a combination of mass spectrometry and UV-vis spectroscopy in comparison with an authentic sample, synthesized directly by an independent procedure using Fe(ClO)·HO.

A Pot-Economical Approach to the Total Synthesis of Sch-725674.

A pot-economical total synthesis of antifungal Sch-725674, 1, is reported. The approach takes advantage of a number of one-pot, sequential transformations, including a phosphate tether-mediated one-pot, sequential RCM/CM/chemoselective hydrogenation protocol, a one-pot tosylation/acrylation sequence, and a one-pot, sequential Finkelstein reaction/Boord olefination/acetonide deprotection procedure to streamline the synthesis route by reducing isolation and purification procedures, thus saving time. Overall, an asymmetric route has been developed that is efficiently accomplished in seven pots from phosphate (S,S)-triene and with minimal purification.

Retrospective analysis of the clinical and demographic variables on the outcomes after second-line treatment in advanced non-small cell lung cancer.

Background: Platinum based doublets chemotherapy are the standard of care for metastatic or advanced non-small cell lung carcinoma. This leads to modest survival advantage and improve quality-of-life. However, patients with advanced or metastatic disease eventually present disease progression and needs second-line systemic therapy in a selected group of patients or other supportive measures.

Hydroxylated analogues of the orally active broad spectrum antifungal, Sch 51048 (1), and the discovery of posaconazole [Sch 56592; 2 or (S,S)-5].

As part of a detailed study, the syntheses, biological activities, and pharmacokinetic properties of hydroxylated analogues of the previously described broad spectrum antifungal agents, Sch 51048 (1), Sch 50001 (3), and Sch 50002 (4), are described. Based on an overall superior profile, one of the alcohols, Sch 56592 (2), was selected for clinical studies.

Profile of non-compressive myelopathy in eastern India: a 2-year study.

Eighty-two patients with non-compressive myelopathy have been studied from July 1994 to June 1996 in Bangur Institute of Neurology and S.S.K.