Discussion of “Risk Analysis of Traffic and Revenue Forecasts for Road Investment Projects” by Arun Kumar, M. L. Kansal, V. K. Minocha, and Sanjay Kumar

The isatin framework is a useful template for the development of novel anticancer agents. This is exemplified by the fact that several isatin‐based anticancer agents, such as semaxanib, sunitinib, nintedanib, and hesperadin, are already in use or under clinical trials for the treatment of diverse kinds of cancers. Isatin‐based hybrids could be obtained by incorporating other anticancer pharmacophores into the isatin skeleton and they have the potential to overcome drug resistance with reduced side effects. Thus, isatin‐based hybrids may provide attractive scaffolds for the development of novel anticancer agents. This review covers the recent advances of isatin‐based hybrids with anticancer activity, covering articles published between 2001 and 2019. The anticancer activities of these molecules and the structure–activity relationships are also discussed. The purpose of this review article is to set up the direction for the design and development of isatin‐based hybrids with high efficacy and low toxicity.

Section: Isatin-azole Hybridsmentioning

confidence: 99%

“…Further study indicated that the bis-isatin-bis-1,2,3-triazole-uracil hybrids 35 (IC 50 : 13.90 to >100 μM, MTT assay) only displayed weak to moderate activity against HeLa, MCF-7, and DU145 cancer cell lines. [89] Six isatin-1,2,4-triazole-isatin hybrids 36 (IC 50 :…”

Section: Isatin-azole Hybridsmentioning

confidence: 99%

Recent advances in isatin hybrids as potential anticancer agents

Ding

Zhou

Zeng

2020

“…The β-lactam-containing chalcone-ferrocene hybrids 14 and 15 showed higher activity against the CQR W2 strain (IC 50 : 2.89-16.79 μM and 2.36-26.92 μM, respectively) compared with the CQS 3D7 strain (IC 50 : 5.81-34.67 μM and 4.80 to >100 μM, respectively), suggesting that these hybrids may have the potential to treat drug-resistant malaria. [45] The SAR revealed that the nature of the substituent at the N−1 position of β-lactam influenced the activity greatly. Hybrids with cycloalkyl groups were more potent than their phenyl ring analogs, while the length of alkyl chain had little impact.…”

Section: Of 10mentioning

confidence: 99%

Chalcone hybrids and their antimalarial activity

Cheng

Yang

Huang

et al. 2020

Malaria, one of the most striking, re‐emerging infectious diseases caused by the genus Plasmodium, places a huge burden on global healthcare systems. A major challenge in the control and eradication of malaria is the continuous emergence of increasingly widespread drug‐resistant malaria, creating an urgent need to develop novel antimalarial agents. Chalcone derivatives are ubiquitous in nature and have become indispensable units in medicinal chemistry applications due to their diverse biological profiles. Many chalcone derivatives demonstrate potential in vitro and in vivo antimalarial activity, so chalcone could be a useful template for the development of novel antimalarial agents. This review covers the recent development of chalcone hybrids as antimalarial agents. The critical aspects of the design and structure–activity relationship of these compounds are also discussed.

“…[63] Further study indicated that the isatin-1,2,3-triazole-uracil-1,2,3triazole-isatin hybrids 25 ( Figure 5; IC 50 : 13.90 to >100 μM, MTT assay) only displayed weak to moderate activity against HeLa, MCF-7, and DU145 cancer cell lines. [64] However, removal of the 1,2,3-triazole moiety was also tolerated, and diethylene glycol-tethered isatin dimers 26 (IC 50 : 8.32-49.73 μM, SRB assay) showed considerable activity against HepG2, HeLa, A549, DU145, SKOV3, MCF-7, and drugresistant MCF-7/DOX cancer cell lines. [65] Halogen atoms at the C-5 position of isatin skeleton were harmful to the activity, whereas oxime and semicarbazone at C-3 position could boost up the activity.…”

Section: Replacement Of the Diethylene/tetraethylene Glycol Linker Bymentioning

confidence: 99%

Isatin dimers and their biological activities

Zhang

Liu

et al. 2020

Dimerization is a promising strategy to develop novel drug candidates that could extend the biological spectrum, enhance the activity, overcome drug resistance, as well as improve pharmacological, pharmacokinetic, and physicochemical profiles. Isatin dimers possess a broad spectrum of biological properties and the isatin dimer indirubin has already been used in the clinic, revealing the potential of isatin dimers as putative drugs. This review covers the recent advances of isatin dimers as pharmacologically significant scaffolds and the structure–activity relationship to set up the direction for the design and development of isatin dimers with higher efficiency and lower toxicity.