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» Authors » Aranapakam M Venkatesan

Aranapakam M Venkatesan

Explore the profile of Aranapakam M Venkatesan including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 27
Citations 320
Followers 0
Related Specialties
Chemistry
Biochemistry
Pharmacology
Top 10 Co-Authors
Tarek S Mansour
Semiramis Ayral-Kaloustian
Zecheng Chen
Osvaldo dos Santos
Takao Abe
Judy Lucas
Christoph M Dehnhardt
Irwin Hollander
Efren Delos Santos
Natasja Brooijmans
Published In
J Med Chem
Bioorg Med Chem Lett
Antimicrob Agents Chemother
Bioorg Med Chem
J Org Chem
Affiliations
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Recent Articles
1.
Ultrasmall Folate Receptor Alpha Targeted Enzymatically Cleavable Silica Nanoparticle Drug Conjugates Augment Penetration and Therapeutic Efficacy in Models of Cancer
Wu F, Chen P, Gardinier T, Turker M, Venkatesan A, Patel V, et al.
ACS Nano . 2022 Oct; 16(12):20021-20033. PMID: 36264003
To address the key challenges in the development of next-generation drug delivery systems (DDS) with desired physicochemical properties to overcome limitations regarding safety, in vivo efficacy, and solid tumor penetration,...
2.
Synthetic Study toward Total Synthesis of (±)-Germine: Synthesis of (±)-4-Methylenegermine
Stork G, Yamashita A, Hanson R, Phan L, Phillips E, Dube D, et al.
Org Lett . 2017 Sep; 19(19):5150-5153. PMID: 28876074
The total synthesis of 4-methylenegermine is described.
3.
Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors
Dehnhardt C, Venkatesan A, Chen Z, Delos-Santos E, Ayral-Kaloustian S, Brooijmans N, et al.
Bioorg Med Chem Lett . 2011 Jul; 21(16):4773-8. PMID: 21763134
We recently described several highly potent, triazine (1) and triazolopyrimidine (2) scaffold-based, dual PI3K/mTOR-inhibitors (e.g., 1, PKI-587) that were efficacious in both in vitro and in vivo models. In order...
4.
PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor
Venkatesan A, Chen Z, dos Santos O, Dehnhardt C, Santos E, Ayral-Kaloustian S, et al.
Bioorg Med Chem Lett . 2010 Aug; 20(19):5869-73. PMID: 20797855
A series of mono-morpholino 1,3,5-triazine derivatives (8a-8q) bearing a 3-oxa-8-azabicyclo[3.2.1]octane were prepared and evaluated for PI3-kinase/mTOR activity. Replacement of one of the bis-morpholines in lead compound 1 (PKI-587) with 3-oxa-8-azabicyclo[3.2.1]octane...
5.
5-ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-alpha and mTOR for the treatment of breast cancer
Zhang N, Ayral-Kaloustian S, Anderson J, Nguyen T, Das S, Venkatesan A, et al.
Bioorg Med Chem Lett . 2010 May; 20(12):3526-9. PMID: 20483602
A series of 5-ureidobenzofuran-3-one indoles as potent inhibitors of PI3Kalpha and mTOR has been developed. The best potency in cells was obtained when the urea group was extended to a...
6.
Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors
Chen Z, Venkatesan A, Dehnhardt C, Ayral-Kaloustian S, Brooijmans N, Mallon R, et al.
J Med Chem . 2010 Mar; 53(8):3169-82. PMID: 20334367
Significant evidence suggests that deregulation of the PI3K/Akt pathway is important in tumor progression. Mechanisms include loss of function of the tumor suppressor PTEN and high frequency of mutation of...
7.
Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor
Venkatesan A, Dehnhardt C, Santos E, Chen Z, dos Santos O, Ayral-Kaloustian S, et al.
J Med Chem . 2010 Feb; 53(6):2636-45. PMID: 20166697
The PI3K/Akt signaling pathway is a key pathway in cell proliferation, growth, survival, protein synthesis, and glucose metabolism. It has been recognized recently that inhibiting this pathway might provide a...
8.
Stereoselective synthesis of an active metabolite of the potent PI3 kinase inhibitor PKI-179
Chen Z, Venkatesan A, dos Santos O, Santos E, Dehnhardt C, Ayral-Kaloustian S, et al.
J Org Chem . 2010 Feb; 75(5):1643-51. PMID: 20112997
The synthesis and stereochemical determination of 1-(4-(4-((1R,5R,6R)-6-hydroxy-3-oxa-8-azabicyclo[3.2.1]octan-8-yl)-6-morpholino-1,3,5-triazin-2-yl)phenyl)-3-(pyridin-4-yl)urea (2), an active metabolite of the potent PI3 kinase inhibitor PKI-179 (1), is described. Stereospecific hydroboration of the double bond of 2,5-dihydro-1H-pyrrole 8...
9.
Novel benzofuran derivatives with dual 5-HT1A receptor and serotonin transporter affinity
Venkatesan A, Dos Santos O, Ellingboe J, Evrard D, Harrison B, Smith D, et al.
Bioorg Med Chem Lett . 2010 Jan; 20(3):824-7. PMID: 20064720
Several benzofuran derivatives linked to a 3-indoletetrahydropyridine through an alkyl chain were prepared and evaluated for serotonin transporter and 5-HT(1A) receptor affinities. Their design, synthesis and structure-activity relationships are described.
10.
Design and synthesis of novel diaminoquinazolines with in vivo efficacy for beta-catenin/T-cell transcriptional factor 4 pathway inhibition
Dehnhardt C, Venkatesan A, Chen Z, Ayral-Kaloustian S, dos Santos O, Santos E, et al.
J Med Chem . 2009 Dec; 53(2):897-910. PMID: 20025292
We are introducing a novel series of 2,4-diaminoquinazolines as beta-catenin/Tcf4 inhibitors which were identified by ligand-based design. Here we elucidate the SAR of this series and explain how we were...