Susanta Samajdar
Research Director at Aurigene Discovery Technologies
Aurigene Discovery Technologies Limited
39-40, KIADB Industrial Area Electronic City Ph II, Hosur Road
Bangalore , Karnataka 560100
India
Susanta Samajdar, Ph.D., Research Director, Medicinal Chemistry, Aurigene Discovery Technologies Limited
Susanta Samajdar received his Ph.D. in Synthetic Organic Chemistry from Indian Association for the Cultivation of Science (IACS), Kolkata and subsequently moved to MD Anderson Cancer Center for a Post-Doctoral training on anti-cancer drug discovery.
He has over 12 years of synthetic and Medicinal Chemistry research experience in Indian Industries.
Susanta has experience in leading
multi-disciplinary drug discovery teams that successfully delivered
several preclinical development candidates.
He has elaborate experience in working with Kinases
and other target classes like GPCRs, Ion channels, Proteases and NHRs,
across different therapeutic areas like Oncology, Pain and Inflammation
and Neurosciences.
links
https://www.facebook.com/susanta.samajdar
https://www.researchgate.net/profile/Susanta_Samajdar
https://profiles.google.com/114544433547394350208/about
https://in.linkedin.com/in/susanta-samajdar-b6025821
http://selectbioindia.net/proceedings/Report%20MCI2015.pdf
Susanta Samajdar, Research Director, Aurigene Discovery Technologies Limited
Dr. Susanta Samajdar received his PhD in Synthetic Organic Chemistry from Indian Association for the Cultivation of Science (IACS), Kolkata and subsequently moved to MD Anderson Cancer Center for a Post-Doctoral Research on anti-cancer drug discovery. He has over 15 years of synthetic and Medicinal Chemistry research experience in Indian Industries. Susanta has experience in leading multi-disciplinary drug discovery teams that successfully delivered several preclinical development candidates. He has experience in working with various target classes including GPCRs, Ion channels, Proteases, Kinases, NHRs, Epigenetics etc across different therapeutic areas like Oncology, Pain and Inflammation, Metabolic Disorders and Neurosciences. He has more than 20 publications and several patents to his credit.Experience
Research Director in Medicinal Chemistry
Aurigene Discovery Technologies
Associate Director
Jubilant Biosys
Drug Discovery Medicinal Chemistry
Education
-
10:50 Novel IRAK4 Inhibitors for Oncology and Inflammation
Susanta Samajdar, Ph.D., Research Director, Medicinal Chemistry, Aurigene Discovery Technologies Limited
This presentation will discuss the discovery and optimization of hit series, some preliminary in vivo data, combination therapy strategy, present focus and further advancements.
Simple Synthesis of Substituted Pyrroles†
The
University of Texas, M. D. Anderson Cancer Center, Department of
Molecular Pathology, Box 89, 1515 Holcombe Boulevard, Houston, Texas
77030 %bbanik@mail.mdanderson.org
J. Org. Chem., 2004, 69 (1), pp 213–216
DOI: 10.1021/jo035200i, http://pubs.acs.org/doi/abs/10.1021/jo035200i?journalCode=joceah
Bimal K. Banik, Anjan Ghatak, , Manas K. Basu, Linda Hackfeld, Indrani Banik, Oliwia Zegrocka, Frederick F. Becker
Abstract C190: Potent and selective inhibition of CDK7 by novel covalent inhibitors
- Ramulu Poddutoori,
- Leena K. Satyam,
- Girish Daginakatte,
- Subhendu Mukherjee,
- Sivapriya Marappan,
- Sreevalsam Gopinath,
- Raghuveer Ramachandra,
- Anirudha Lakshminarasimhan,
- Manoj Pothuganti,
- Shilpa Nayak,
- Nandish C,
- Chandranath Naik,
- Ravindra MV,
- Madhu Dabbeeru,
- Thomas Antony,
- Chetan Pandit,
- Murali Ramachandra,
- Shekar Chelur, and
- Susanta Samajdar
+ Author Affiliations
Abstracts: AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; November 5-9, 2015; Boston,
MA
Abstract
Cyclin-dependent kinase 7 (CDK7) is an
important constituent of the cellular transcriptional machinery, where
it phosphorylates
the C-terminal domain (CTD) of RNAP polymerase II
(RNAPII). Because many tumor types are critically dependent on
transcription
for maintenance of their oncogenic state,
pharmacological modulation of CDK7 kinase activity is considered as an
approach
to treat cancer. Multiple series of CDK7 inhibitors
were identified by iterative medicinal chemistry efforts and SAR based
approach. Early compounds were optimized towards
attaining good physicochemical properties, high potency, good
selectivity
and desirable pharmacokinetic profile to achieve
anti-tumor activity. We have identified compounds from two distinct
chemical
series that are highly potent in inhibiting CDK7 in
biochemical assays. These inhibitors demonstrate time-dependent
inhibition
of CDK7 indicating covalent nature of binding. The
compounds showed potent anti-proliferative activity in cell lines
derived
from various tumor types and this was accompanied
by CDK7 modulation in cells as monitored by pS5RNAPII levels. They have
excellent drug-like characteristics including
solubility, permeability, metabolic stability and good oral
bioavailability.
In a broad panel of kinases (332 kinase), selected
compounds from both series showed good selectivity profile. Tolerability
and efficacy studies are ongoing with selected
early leads to test their impact on tumor growth inhibition in xenograft
models.
We have identified novel and selective CDK7
covalent inhibitors from two series with desirable drug-like properties,
which
are being evauated for anti-tumor activity in
xenograft models.
Citation Format: Ramulu
Poddutoori, Leena K. Satyam, Girish Daginakatte, Subhendu Mukherjee,
Sivapriya Marappan, Sreevalsam Gopinath, Raghuveer
Ramachandra, Anirudha Lakshminarasimhan, Manoj
Pothuganti, Shilpa Nayak, Nandish C, Chandranath Naik, Ravindra MV,
Madhu Dabbeeru,
Thomas Antony, Chetan Pandit, Murali Ramachandra,
Shekar Chelur, Susanta Samajdar. Potent and selective inhibition of CDK7
by novel covalent inhibitors. [abstract]. In:
Proceedings of the AACR-NCI-EORTC International Conference: Molecular
Targets
and Cancer Therapeutics; 2015 Nov 5-9; Boston, MA.
Philadelphia (PA): AACR; Mol Cancer Ther 2015;14(12 Suppl 2):Abstract nr
C190.
Event Abstract
Discovery of potent and selective retinoid related orphan receptor gamma (RORγ) inverse agonists for the treatment of Th17 mediated diseases
- 1 Aurigene Discovery Technologies Ltd., India
Background: Th17 cells play a key pro-inflammatory role in a variety of autoimmune diseases. The nuclear hormone receptor RORγ controls the differentiation of Th17 cells and expression of IL-17.
Methods: Novel RORγ inverse agonists were designed using structure and knowledge based methods. Compounds were screened in a RORγ radio-ligand binding assay using 3H 25- Hydroxycholesterol, as well as in a cell based reporter assay to demonstrate inverse agonism. Selected compounds were screened against RORα to evaluate selectivity. Crystal structure of RORγ in complex with known inverse agonists as well as novel compounds, were solved. Th17 differentiation assay was developed using primary mouse CD4+ve T-cells to determine functional effect of the compounds. Pharmacokinetic profile in mice was determined for selected compounds.
Results: Novel hits from multiple structural classes have been identified, with IC50 in the range of 5 – 500 nM in binding assay. Compounds from the lead series demonstrated good activity (< 1 μM) in reporter assay. Co-crystal structure of novel compounds clearly showed the mode of binding. Several compounds demonstrated > 10 fold selectivity against RORα in a reporter assay. Compounds from multiple series have shown significant inhibition of IL-17 release from differentiated Th17 cells. Lead compounds have shown good pharmacokinetic properties in mice.
Conclusions: We have identified novel and structurally diverse small molecule inverse agonists of
RORγ. Selectivity against RORα and cell based activity has been demonstrated for compounds from multiple series. Relevant efficacy models have been established and profiling of lead compounds in these models in on-going.
Methods: Novel RORγ inverse agonists were designed using structure and knowledge based methods. Compounds were screened in a RORγ radio-ligand binding assay using 3H 25- Hydroxycholesterol, as well as in a cell based reporter assay to demonstrate inverse agonism. Selected compounds were screened against RORα to evaluate selectivity. Crystal structure of RORγ in complex with known inverse agonists as well as novel compounds, were solved. Th17 differentiation assay was developed using primary mouse CD4+ve T-cells to determine functional effect of the compounds. Pharmacokinetic profile in mice was determined for selected compounds.
Results: Novel hits from multiple structural classes have been identified, with IC50 in the range of 5 – 500 nM in binding assay. Compounds from the lead series demonstrated good activity (< 1 μM) in reporter assay. Co-crystal structure of novel compounds clearly showed the mode of binding. Several compounds demonstrated > 10 fold selectivity against RORα in a reporter assay. Compounds from multiple series have shown significant inhibition of IL-17 release from differentiated Th17 cells. Lead compounds have shown good pharmacokinetic properties in mice.
Conclusions: We have identified novel and structurally diverse small molecule inverse agonists of
RORγ. Selectivity against RORα and cell based activity has been demonstrated for compounds from multiple series. Relevant efficacy models have been established and profiling of lead compounds in these models in on-going.
Keywords:
RORγ,
Autoimmune Diseases,
Th17 Cells,
IL-17,
Psoriasis
Conference:
15th International Congress of Immunology (ICI), Milan, Italy, 22 Aug - 27 Aug, 2013.
Presentation Type:
Abstract
Topic:
Immune-mediated disease pathogenesis
Citation:
Nellore
K,
Bejugam
M,
Ramanathan
A,
Mukherjee
S,
Lakshminarasimhan
A,
Dodheri
SS,
Rao
N,
Damarla
R,
Samajdar
S and
Subramanya
H
(2013). Discovery of potent and selective retinoid related orphan receptor gamma (RORγ) inverse agonists for the treatment of Th17 mediated diseases.
Front. Immunol.
Conference Abstract:
15th International Congress of Immunology (ICI).
doi: 10.3389/conf.fimmu.2013.02.00678
Received:
13 Jun 2013;
Published Online:
22 Aug 2013.
*
Correspondence:
Dr. Hosahalli Subramanya, Aurigene Discovery Technologies Ltd., Bangalore, India, hosahalli_s@aurigene.comAsymmetric synthesis of anticancer β-lactams via Staudinger reaction
- Authors:
- Bimal K. Banik
- Susanta Samajdar
- Frederick F. Becker
- View Affiliations
-
Published online on: Monday, March 1, 2010
- Pages: 319-321 DOI: 10.3892/mmr_00000259
Abstract
This study describes the symmetric synthesis of novel β-lactams derived
from chrysene directed towards their SAR, as well as their biological
activities against several cancer cell lines in vitro. To our knowledge,
this is the first report on the synthesis and biological evaluation of
optically active anticancer β-lactams. That these anticancer effects are
not uniform against all tumor lines suggests that the target of the
action of these compounds is highly specific.
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