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Santosh Kumar Guru

National Institute of Pharmaceutical Education and Research

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Shashi Bhushan

University of Lucknow

Ram A. Vishwakarma

Council of Scientific and Industrial Research

Anup S. Pathania

University of Nebraska Medical Center

Fayaz Malik

Indian Institute of Integrative Medicine

Srushti Mahajan

National Institute of Pharmaceutical Education and Research

Pankaj Kumar Singh

National Institute of Pharmaceutical Education and Research

Sandip B. Bharate

Indian Institute of Integrative Medicine

Shreyans K. Jain

Banaras Hindu University

Ujala Gupta

National Institute of Pharmaceutical Education and Research

Mayur Aalhate

National Institute of Pharmaceutical Education and Research

Cooperative Institutions

Indian Institute of Integrative Medicine

Academy of Scientific and Innovative Research

National Institute of Pharmaceutical Education and Research

Council of Scientific and Industrial Research

University of Jammu

National Institute of Pharmaceutical Education and Research

Banaras Hindu University

Institute of Minerals and Materials Technology

Indian Institute of Technology BHU

Institute of Medical Sciences

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Data from Secalonic Acid-D Represses HIF1α/VEGF-Mediated Angiogenesis by Regulating the Akt/mTOR/p70S6K Signaling Cascade

Santosh Kumar Guru Anup S. Pathania Suresh Kumar Ramesh Deshidi Manjeet Kumar

<div>Abstract<p>Tumor angiogenesis is a validated target for therapeutic intervention, but agents that are more disease selective are needed. Here, we report the isolation of secalonic acid-D (SAD), a mycotoxin from a novel source that exhibits potent antiangiogenic antitumor activity. SAD inhibited multiple HIF1α/VEGF-arbitrated angiogenesis dynamics as scored in human umbilical vascular endothelial cells and human MCF-7 breast tumor xenografts. Similarly, SAD suppressed VEGF-induced microvessel sprouting from rat aortic ring and blood vessel formation in the Matrigel plug assay in C57/BL6J mice. Under normoxic or hypoxic conditions, SAD inhibited cell survival through the Akt/mTOR/p70S6K pathway, with attendant effects on key proangiogenesis factors, including HIF1α, VEGFR, and MMP-2/MMP-9. These effects were reversed by cotreatment with the Akt inhibitors perifosine and GSK69069 or by the addition of neutralizing VEGF antibodies. The apoptotic properties of SAD were determined to be both extrinsic and intrinsic in nature, whereas the cell-cycle inhibitory effects were mediated by altering the level of key G<sub>1</sub>–S transition-phase proteins. In experimental mouse models of breast cancer, SAD dosing produced no apparent toxicities (either orally or intraperitoneal) at levels that yielded antitumor effects. Taken together, our findings offered a preclinical validation and mechanistic definition of the antiangiogenic activity of a novel mycotoxin, with potential application as a cancer-selective therapeutic agent. <i>Cancer Res; 75(14); 2886–96. ©2015 AACR</i>.</p></div>

10.1158/0008-5472.c.6506963

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CCDC 2289770: Experimental Crystal Structure Determination

The Cambridge Structural Database (2023)

Rupali Mahajan Abhishek Sharma B. B. PATRA Lijo Mani Parul Grover

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.

10.5517/ccdc.csd.cc2gvpkl

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Mahamanalactone A, a new triterpenoid from Dysoxylum malabaricum bark: a case study for rapid identification of new metabolites via LC-HRMS profiling and database mining strategy

Natural Product Research (2024)

Nivedita Bhardwaj S. Swathilakshmi Nancy Tripathi Sanjay Kumar Uma Ranjan Lal

In this recent investigation, the focus centred on exploring the potential phytoconstituents within the bark of Dysoxylum malabaricum. A profiling strategy employing LC-HRMS (Liquid Chromatography-High Resolution Mass Spectrometry) was implemented for the rapid identification of compounds from the bark extract. The crude extract underwent fractionation, resulting in the isolation of four previously known compounds (1–4) and a novel cycloartane triterpenoid named Mahamanalactone A (5). Compound 5 represents a cycloartane triterpenoid with a modified ring-A, featuring £-caprolactone fusion at positions 4 and 5, distinguishing it from other reported compounds where £-caprolactone is typically fused at positions 3 and 4. Cytotoxicity assessment revealed that the newly identified compound 5 exhibited a moderate cytotoxic profile (IC50 29 to 78 µM) against a panel of cancer cell lines.

Cancer cell lines

10.1080/14786419.2023.2298721

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Combination of docetaxel and newly synthesized 9-Br-trimethoxybenzyl-noscapine improve tubulin binding and enhances antitumor activity in breast cancer cells

Computers in Biology and Medicine (2021)

Shruti Gamya Dash Srinivas Kantevari Santosh Kumar Guru Pradeep Kumar Naik

Noscapine

10.1016/j.compbiomed.2021.104996

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Synthesis and anti-proliferative activities of new derivatives of embelin

Bioorganic & Medicinal Chemistry Letters (2014)

Baljinder Singh Santosh Kumar Guru Rashmi Sharma Sonali S. Bharate Inshad Ali Khan

Piperidine

Mannich reaction

Mannich base

10.1016/j.bmcl.2014.08.052

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A novel triazole derivative of betulinic acid induces extrinsic and intrinsic apoptosis in human leukemia HL-60 cells

European Journal of Medicinal Chemistry (2015)

Imran Khan Santosh Kumar Guru Santosh Kumar Rath Praveen K. Chinthakindi Buddh Singh

Betulinic acid

Intrinsic apoptosis

Natural product

Triazole

10.1016/j.ejmech.2015.11.018

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Synthesis of some new N1-[(2-oxo-3-chloro-4-aryl-azitidin)-(acetyl amino)]-indole derivatives and their pharmacological activity

Zenodo (CERN European Organization for Nuclear Research) (2006)

Santosh Kumar Guru Ritu Yadav Soumya Srivastava S. K. Srivastava S. K. Srivastava

Indole on reaction with chloroacetyl chloride afforded N 1 -(1-chloro acetyl)-indole which was refluxed with hydrazine hydrate to give N 1 -[(1-hydrazinolacetyl]-indole. The hydrazino derivative of indole was further treated with various substituted aromatic carbonyls to get N 1 -[(benzylidene hydrazino)-acetyl]-indoles (3a-j). The compounds 3a-j were treated with chloroacetyl chloride in presence of Et 3 N to afford N 1 -[(2-oxo-3-chloro-4-aryl-azitidin)-(acetyl amino)]-indoles, 4a-j. The structures of all the compounds were elucidated by elemental analysis, IR and 1 H NMR spectrometry. All the compounds were screened for their antimicrobial, anti-inflammatory and anticonvulsant activities.

10.5281/zenodo.5834026

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Accommodation of ring C expanded deoxyvasicinone in the HDAC inhibitory pharmacophore culminates into a tractable anti-lung cancer agent and pH-responsive nanocarrier

European Journal of Medicinal Chemistry (2022)

Ram Sharma Esha Chatterjee Jacob Mathew Sachin Sharma N. Vijayakameswara Rao

Nanocarriers

10.1016/j.ejmech.2022.114602

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585: The synthetic Tryptanthrin analogue suppresses STATs signalling and induces caspase dependent apoptosis via ERK up regulation in human leukemia HL-60 cells

European Journal of Cancer (2014)

Anup S. Pathania S Jamuna R Ashok Kumar Santosh Kumar Guru Fayaz Malik Satej Bhushan

Signalling

10.1016/s0959-8049(14)50520-5

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ChemInform Abstract: Synthesis, Antiproliferative and Apoptosis‐Inducing Activity of Thiazolo[5,4‐d]pyrimidines.

ChemInform (2014)

Baljinder Singh Santosh Kumar Guru Smit Kour Shreyans K. Jain Rajni Sharma

Abstract 14 Title compounds of type (V) are prepared and tested for their antiproliferative and apoptosis‐inducing activities.

10.1002/chin.201420162

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