Management of Pests of Oilseed Crops

Basappa, H.; Duraimurugan, P.

doi:10.1007/978-981-10-8687-8_8

Cited by 10 publications

(10 citation statements)

References 2 publications

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“…Strikingly, treatment with compound 4-MMI resulted in a profound inhibition of tumor growth and burden in the aggressive MPC-11 myeloma (Figure 5). We also noted a profound reduction in VEGF levels in tumor sections derived from 4-MMI treated vs. untreated mice, likely due to inhibition of heparanasemediated VEGF gene expression and/or release [6,7,10]. Due to limited amounts of the 4-MMI compound, we could not perform dose-response and pharmacokinetic studies.…”

Section: Discussionmentioning

confidence: 87%

“…Although there are only two repeating sugar units, they exhibit broad diversity in structure generated by a complex pattern of deacetylation, sulfation, and epimerization [3]. Importantly, the sulfated regions of HS serve as docking sites for ECM components, extrinsic proteins, growth-promoting factors (i.e., VEGF, FGF, HGF, TGFβ), chemokines, and cytokines [4,5], indicating that HSPG is crucial in maintaining tissue/cell architecture, growth, and differentiation [3,6]. Heparanase is the only β-endoglycosidase that partially degrades the HS saccharide side chains of HSPG to generate fragments of 4-7 kDa in length [7][8][9].…”

Section: Introductionmentioning

confidence: 99%

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New Heparanase-Inhibiting Triazolo-Thiadiazoles Attenuate Primary Tumor Growth and Metastasis

Barash

Rangappa²,

Mohan

et al. 2021

Cancers

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Compelling evidence ties heparanase, an endoglycosidase that cleaves heparan sulfate side (HS) chains of proteoglycans, with all steps of tumor development, including tumor initiation, angiogenesis, growth, metastasis, and chemoresistance. Moreover, heparanase levels correlate with shorter postoperative survival of cancer patients, encouraging the development of heparanase inhibitors as anti-cancer drugs. Heparanase-inhibiting heparin/heparan sulfate-mimicking compounds and neutralizing antibodies are highly effective in animal models of cancer progression, yet none of the compounds reached the stage of approval for clinical use. The present study focused on newly synthesized triazolo–thiadiazoles, of which compound 4-iodo-2-(3-(p-tolyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-6-yl)phenol (4-MMI) was identified as a potent inhibitor of heparanase enzymatic activity, cell invasion, experimental metastasis, and tumor growth in mouse models. To the best of our knowledge, this is the first report showing a marked decrease in primary tumor growth in mice treated with small molecules that inhibit heparanase enzymatic activity. This result encourages the optimization of 4-MMI for preclinical and clinical studies primarily in cancer but also other indications (i.e., colitis, pancreatitis, diabetic nephropathy, tissue fibrosis) involving heparanase, including viral infection and COVID-19.

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Section: Discussionmentioning

confidence: 87%

Section: Introductionmentioning

confidence: 99%

New Heparanase-Inhibiting Triazolo-Thiadiazoles Attenuate Primary Tumor Growth and Metastasis

Barash

Rangappa²,

Mohan

et al. 2021

Cancers

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“…The sulfonamide moiety is a common building block in organic synthesis [1][2][3][4][5][6][7][8][9][10][11][12][13][14] and an essential functional group in drug design. [15][16][17][18][19] Sulfonamides have a wide range of medical applications due to their anti-inflammatory, [15][16][17] antibacterial, [18][19][20][21] antimicrobial, [22][23][24] anticancer, [25][26][27][28][29][30][31] antimalarial, 32 and antipsychotic activities. 33 They have been reported to be inhibitors of DNA double-strand break repair, 34 dual angiotensin II and endothelin A receptor antagonists, 35 cyclooxygenase-2 inhibitors associated with different diseases, [36][37][38][39][40][41][42]…”

Section: Application Of Sulfonamidesmentioning

confidence: 99%

Recent Functionalizations of Primary Sulfonamides

Chen

2016

Synthesis

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Sulfonamides are common building blocks in organic synthesis. They have a wide range of medical applications. This review aims to delineate recent efforts towards the functionalization of primary sulfonamides during last three years and to provide an overview of the synthesis of N-alkylated, N-acylated, and N-arylated sulfonamides from primary sulfonamides. Among other reactions, the sulfonamide-directed C-H functionalization is highlighted.

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“…Recently, compound 2 (Figure 1) was also reported to inhibit the autophagy activating kinase 1 (ULK1) with an IC 50 of 14 nM, and ULK1/2 inhibition in combination with Olaparib [21]. In continuation of the effort in the synthesis of novel oxadiazoles [22][23][24][25][26][27][28], herein synthesis of oxadiazoles with substitutions of pyridine, biphenyl, pyrimidine, and thiophene rings that target PARP1 and the efficacy of these compounds in BRCA wild-type estrogen receptor positive (ER+) and triple-negative breast cancer (TNBC) cells is reported.…”

Section: Introductionmentioning

confidence: 99%

Design and Activity of Novel Oxadiazole Based Compounds That Target Poly(ADP-ribose) Polymerase

et al. 2022

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Novel PARP inhibitors with selective mode-of-action have been approved for clinical use. Herein, oxadiazole based ligands that are predicted to target PARP-1 have been synthesized and screened for the loss of cell viability in mammary carcinoma cells, wherein seven compounds were observed to possess significant IC50 values in the range of 1.4 to 25 µM. Furthermore, compound 5u, inhibited the viability of MCF-7 cells with an IC50 value of 1.4µM, when compared to Olaparib (IC50 = 3.2 µM). Compound 5s also decreased cell viability in MCF-7 and MDA-MB-231 cells with IC50 values of 15.3 and 19.2 µM, respectively. Treatment of MCF-7 cells with compounds 5u and 5s produced PARP cleavage, H2AX phosphorylation and CASPASE-3 activation comparable to that observed with Olaparib. Compounds 5u and 5s also decreased foci-formation and 3D Matrigel growth of MCF-7 cells equivalent to or greater than that observed with Olaparib. Finally, in silico analysis demonstrated binding of compound 5s towardsthe catalytic site of PARP-1, indicating that these novel oxadiazoles synthesized herein may serve as exemplars for the development of new therapeutics in cancer.

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Management of Pests of Oilseed Crops

Cited by 10 publications

References 2 publications

New Heparanase-Inhibiting Triazolo-Thiadiazoles Attenuate Primary Tumor Growth and Metastasis

New Heparanase-Inhibiting Triazolo-Thiadiazoles Attenuate Primary Tumor Growth and Metastasis

Recent Functionalizations of Primary Sulfonamides

Design and Activity of Novel Oxadiazole Based Compounds That Target Poly(ADP-ribose) Polymerase

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