• भारत सरकार के विज्ञान एवम प्रौदयोगिकी मंत्रालय के जैव प्रौदयोगिकी विभाग की स्वायत्त संस्थान
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Publication

Recent Publications:

  • Direct Conversion of Carboxylic Acids to Various Nitrogen Containing Compounds in One-Pot Exploiting Curtius Rearrangement Arun Kumar, Naveen Kumar, Ritika Sharma, Gaurav Bhargava and Dinesh Mahajan* Journal of Organic Chemistry 2019, 84, 17, 11323-11334 (IF 4.89)
  • Recent Advances in the Development of Integrase Inhibitors for HIV Treatment  J Trivedi, Dinesh Mahajan, RJ Jaffe, A Acharya, D Mitra, SN Byrareddy Current HIV/AIDS Reports 17 (1), 63-75 (IF 4.2)
  • Musa balbisiana Fruit Rich in Polyphenols Attenuates Isoproterenol-Induced Cardiac Hypertrophy in Rats via Inhibition of Inflammation and Oxidative Stress Sima Kumari, Parmeshwar B Katare, R Elancheran, Hina L Nizami, Bugga Paramesha, Sudheer Arava, Partha Pratim Sarma, Roshan Kumar, Dinesh Mahajan, Yashwant Kumar, Rajlakshmi Devi, Sanjay K Banerjee Oxidative Medicine and Cellular Longevity 2020, Just Accepted (IF 4.8)
  • Nickel (0)-Catalyzed [3+ 2]-Cycloadditions of Bis (alkylidenecyclopropanes) with Diazenes: A Facile Synthesis of Functionalized Pyrazolidine-1, 2-dicarboxylates B Kuila, R Naikoo, D Mahajan, P Singh, G BhargavaSynlett 2000 31 (01), 65-68 (IF 2.3)
  • 11-β-hydroxysterols as possible endogenous stimulators of mitochondrial biogenesis as inferred from epicatechin molecular mimicry S Dugar, F Villarreal, FH Hollinger, D Mahajan, I Ramirez-Sanchez, Pharmacological research 2000 151, 104540 (IF 4.5)
  • NU-6027 inhibits growth of Mycobacterium tuberculosis by targeting Protein Kinase D and Protein Kinase GSaqib Kidwai, Rania Bouzeyen, Sohini Chakraborti, Neha Khare, Sumana Das, Tannu Priya Gosain, Assirbad Behura, Chhuttan Lal Meena, Rohan Dhiman, Makram Essafi, Avinash Bajaj, Deepak Kumar Saini, Narayanaswamy Srinivasan, Dinesh Mahajan, Ramandeep Singh Antimicrobial Agents and Chemotherapy 2019, DOI: 10.1128/AAC.00996-19. (IF 5.27)

Publications in 2018:

  • Electrophilic activation of carboxylic anhydrides for nucleophilic acylation reactionsVarun Kumar, Anil Rana, Chhuttan Lal Meena, Nidhi Sharma, Yashwant Kumara & Dinesh Mahajan* Synthesis 2018; Accepted. (IF 2.7);  https://www.thieme-connect.com/products/ejournals/abstract/10.1055/s-0037-1609564
  • A practically simple, catalyst free and scalable synthesis of N-substituted ureas in water; Lata Tiwari, Varun Kumar, Bhuvesh Kumar and Dinesh Mahajan*;  RSC ADV 8 (38), 21585-21595. (IF 3.1); https://pubs.rsc.org/en/content/articlehtml/2018/ra/c8ra03761b
  • Triflic anhydride promoted synthesis of primary amides and their conversion to nitriles; Anil Rana, Varun Kumar, Lata Tiwari, Anamika Thakur, Chhuttan Lal Meena, Dinesh Mahajan* SynOpen 2 (02), 0180-01912018; https://www.thieme-connect.com/products/ejournals/html/10.1055/s-0037-1610154
  • Spermine detection from urine and blood serum using ionic self-assembly of benzimidazolium based dipod and dodecylsulfate; Neetu Tripathia, Prabhpreet Singha, Vijay Luxamib, Dinesh Mahajan, Subodh Kumar Sensors and Actuators B: Chemical 2018, 552-561.(IF 5.1); https://www.sciencedirect.com/science/article/pii/S0925400518309523
  • Acetylenic Ester Promoted Tandem Ring Opening and Cyclizations of Dienyl Thiazolidin-4-ones: A Facile and Chemoselective Synthesis of Functionalized Pyridine-2-Carboxylates Bilash Kuila, Dinesh Mahajan, Kapil Kumar, Prabhpreet Singh, Gaurav Bhargava; Synlett 2018; 29(04): 509-512. (IF 2.3)

Publications before 2018:

  • Killing Glioma 'Stem-like' Cells via Drug-Induced Relocation of Endosomal Urokinase Proteins Fredric A Gorin, Nagarekha Pasupuleti, Dinesh Mahajan, Sundeep Dugar; Jun 2016 · Anti-cancer agents in medicinal chemistry. (IF 2.8)
  • A Facile and Chemoselective Synthesis of 1,4-Benzodiazepin-2-ones and Dienyl Thiazolidin-4-onesBilash Kuila, Yogesh Kumar, DineshMahajan, Prabhpreet Singh, Pankaj, Gaurav Bhargava;  RSC Adv., 2016,6, 57485-57489.(IF 3.3).
  • Discovery of Novel and Orally Bioavailable Inhibitors of PI3 Kinase Based on Indazole Substituted Morpholino-Triazines Sundeep Dugar, Frank P. Hollinger, Dinesh Mahajan*, Somdutta Sen, Bilash Kuila, Reena Arora, Yogesh Pawar, Vaibhav Shinde Mahesh Rahinj, Kamal K. Kapoor, Rahul Bhumkar, Santosh Rai, and Rakesh KulkarniACS Med. Chem. Letters 2015 ASAP DOI: 10.1021/acsmedchemlett.5b00322; (IF 3.2).
  • New small molecules that kill hypoxically transformed glioma stem-like cells Nagarekha Pasupuleti*, Anthony Valenzuela, Yamini Manohar, Dinesh Mahajan, Sundeep Dugar, Jann Sarkaria, Fredric Gorin,  Neuro-Ooncology 17(SUPPL 5):V31-V31 · NOVEMBER 201. (IF 5.56)
  • Preclinical activity of dual PI3K/mTOR inhibitor SPR965 in multiple myeloma Jeremy T. Larsen, Vijay Ramakrishnan, Jessica Haug, Teresa Kimlinger, Somdutta Sen, Dinesh Mahajan, Sundeep Dugar, S. Vincent Rajkumar, Shaji K. Kumar Cancer Research 75(15 Supplement):2653-2653 August 2015; doi: 10.1158/1538-7445.AM2015-2653. (IF 9.33)
  • SPR965: an oral PI3K/ mTOR C1/C2 inhibitor for the treatment of solid tumors Arora,R.; Dutta, B. K.; Goel, R.; Hollinger, F. P.; Kuila, B.; Mahajan, D.; Mahapatra, A. R.; Sagar, M.; Sen, S.; Sharma, A.;  Dugar, S Cancer Res October 1, 2014 74; 4515;doi: 10.1158/1538-7445.AM2014-4515; (IF 9.33)
  • Synthesis and evaluation of pyrrolotriazine based novel small molecules as selective inhibitors for PI3K kinase Sundeep Dugar, Frank Hollinger, Somdutta Sen, Bilash Kuila and Dinesh Mahajan*Bio. Org. Med Chem Letters 2015, 15, 3142. (IF 2.4)
  • A concise and efficient synthetic approach to substituted morpholines. Sundeep Dugar, Amit Sharma, Bilash Kuila and Dinesh Mahajan*, Synthesis 2015, 47, 712-720. (IF 2.7)
  • Nickel catalyzed [3+2] cycloaddition reaction of bis(methylenecyclopropane) with cyclic and acyclic dienophilesBilash Kuila, DineshMahajan, Prabhpreet Singh, Gaurav Bhargava Tetrahedron Letters2015, 56, 1307-1311.(IF 2.4.
  • Metal-free diastereoselective synthesis of diaza-bicyclo[3.2.0]heptan-7-one and its transformation to functionalized proline esters.Yogesh Kumar, Bilash Kuila, DineshMahajan, Prabhpreet Singh, Balaram Mohapatra, Gaurav BhargavaTetrahedron Letters2014, 2793-2795. (IF 2.4)

Inventor in more than 25 filed patent applications. 20 are published online and 15 are issued patents in different jurisdictions (US, China, Europe and Japan).

 

1.     Novel compounds of 11beta-hydroxy-steroids for use in mitochondria biogenesis and diseases associated with mitochondrial dysfunction or depletion, WO/2014/115167; PCT/IN2014/000048; National Phase: China, US, EU and JP.

2.     Novel triazine compounds for Pi3K/mTOR pathway, WO2014016849; PCT/IN2013/000458; CN104582707A, EP2874632A4, GrantedUS14/416,140 dated 25/04/2017;Granted JP6175139B2

3.     Novel triazine compounds, PCTIN2012000055 Granted US13/981,579 dated 1/11/2016

4.     Substituted methylformyl reagents and method of using same to modify physicochemical and/or pharmacokinetic properties of compounds (A new technology patent to address low solubility and bioequivalence of APIs and NCEs), PCTIN2012000248; Granted US14/110,373 dated 07/06/2016; Application pending for grant in China, Europe and Japan

5.     Novel compounds, their preparation and their uses, Granted US14/433,485 Dated 31/01/2017  Pending for Grant in China, Europe and Japan (A new technology patent to address low solubility and bioequivalence of APIs and NCEs).

6.     Methods of treating tumoral diseases, or bacterial or viral infections, PCT US20170000789; US 15266802 Granted US14/046,682 dated 08/11/2016;AU2013326850A US15/266,802 Pending in Japan, Europe and China  

7.     A novel process for synthesis of polyphenols (A process patent for non-infringing route of chiral natural product),  PCT/IN2012/000052; CN103582635A, EP2668176A2, EP2668176A4, US9428482, Granted US13/981,279 Dated 30/08/2016JP5890846B2 Dated 22/03/2016 EP2668176B1;

8.     Novel approach for synthesis of catechins (A process patent for non infringing route for a chiral natural product),  PCT/IN2014/000061; CN105026384A, EP2948437A2, EP2948437A4, US9556140, Granted US14/763,018 Dated 31/01/2017; JP6411375B2

9.     Flavonoid compounds, PCT/US2012/049767;CN103987704A,EP2739613A4, Granted US14/237,167 dated 17/11/2015

10.  Novel compounds, their synthesis and their uses, US09487500

11.  Novel compounds and anti-tubercular agents, PCT/IN2015/000226 Granted US15/313,986dated 2018-10-16. Pending in Russia, Europe, China and Japan

12.  Novel compounds and inhibition of AKT kinase, IN2014DEL237 20140128 

13.  Novel analogues of epicatechin and related polyphenols, PCT/IN2014/000213; CN105283179A, EP2981260A2, EP2981260A4, US20160039781; Granted US14/780,214 Dated 22/05/2018

14.  Method of converting carbon dioxide into carbonyl compounds WO2019073484 (A1) 12 Dec 2017

15.  Hydroxy Steroid Compounds,  their intermediates, process of …US publication number 2015/0376225 A1, Also filed in Europe, China and Japan

16.  Novel molecules and their hiv inhibitory activityIndian Pat. Appl. (2018), IN 201711009180 A 20180921.

Preparation of trigonelline based compounds as API prodrugs PCT Int. Appl. (2017), WO 2017158621 A1 20170921

  1. As PI with Funds as Grants from Govt of India and Industry

    1. Development and PoC validation of a novel approach to treat HIV infection by integrating anti-viral activity with stimulation of host cell innate immunity from DBT-BIRAC under CRS (drug discovery scheme); PI and Project Coordinator;; duration May 2017-May 2020.
    2. Chemical investigation and therapeutic evaluation for linking marker compound(s) with anti-diabetic potential of young shoots of Wendlandia glabrata D.C. and fruits of Phoebe cooperiana, used by indigenous ST people of Arunachal Pradesh.[BT/PR24712/NER/95/828/2017 from DBT- NE Twinning program; 2018-2021.
    3. Structure determination and targeting of ubiquitously expressed membrane integrated form of chloride intracellular channels (CLICs) for discovery of small molecular anti-cancer therapeutics (BT/PR28766/BRB/10/1701/2018). Duration 3 years till Jan 2021

    Industry Funded Project

    1. Penam Laboratories Pvt Ltd, sponsored project for Technology Co-Development (Dec 2018-Oct 2019).

    As Co-PI

    1.  Pharmacological Induction of Autophagy as a Potential Therapeutic Target for Japanese Encephalitis (BT/PR27875/MED/29/1302/2018) from DBT. Duration 3 years till 2021

 

MS.NIDHI SHARMA
TECHNICAL OFFICER-II

DR.NUTAN SHARMA
SERB-TARE FELLOW

MS.PARUL KAMBOJ
ICMR-RESEARCH ASSOCIATE

MR.LALIT MALKANIA
TECHNICAL OFFICER-II

MS.AAKRITI JHA
PROJECT ASSOCIATE-I

The group is looking for PhD candidates with master degree in organic chemistry, medicinal chemistry or pharmcology (MSc or MPharma) to work on drug discovery projects. Email or look for details on THSTI website.

  • 01292876476
  • DINESH[DOT]MAHAJAN[AT]THSTI[DOT]RES[DOT]IN