Synthesis and anticancer activity of new isatin-benzoic acid conjugates

Panga, Shyam; Podila, Naveen Kumar; Asres, Kaleab; Veeresham, Ciddi

doi:10.4314/epj.v31i2.1

Cited by 5 publications

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“…Among all synthesized compounds, 102(b) showed maximum activity on both cell lines. The structure of isatin-based benzoic acid hybrids is given in Figure 97 and in vitro cytotoxicity of compounds 102(a-d) against human cancer cell lines is shown in Table 87 [176].…”

Section: Isatin Containing Hybridsmentioning

confidence: 99%

Concept of Hybrid Drugs and Recent Advancements in Anticancer Hybrids

et al. 2022

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Cancer is a complex disease, and its treatment is a big challenge, with variable efficacy of conventional anticancer drugs. A two-drug cocktail hybrid approach is a potential strategy in recent drug discovery that involves the combination of two drug pharmacophores into a single molecule. The hybrid molecule acts through distinct modes of action on several targets at a given time with more efficacy and less susceptibility to resistance. Thus, there is a huge scope for using hybrid compounds to tackle the present difficulties in cancer medicine. Recent work has applied this technique to uncover some interesting molecules with substantial anticancer properties. In this study, we report data on numerous promising hybrid anti-proliferative/anti-tumor agents developed over the previous 10 years (2011–2021). It includes quinazoline, indole, carbazole, pyrimidine, quinoline, quinone, imidazole, selenium, platinum, hydroxamic acid, ferrocene, curcumin, triazole, benzimidazole, isatin, pyrrolo benzodiazepine (PBD), chalcone, coumarin, nitrogen mustard, pyrazole, and pyridine-based anticancer hybrids produced via molecular hybridization techniques. Overall, this review offers a clear indication of the potential benefits of merging pharmacophoric subunits from multiple different known chemical prototypes to produce more potent and precise hybrid compounds. This provides valuable knowledge for researchers working on complex diseases such as cancer.

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Section: Isatin Containing Hybridsmentioning

confidence: 99%

Concept of Hybrid Drugs and Recent Advancements in Anticancer Hybrids

et al. 2022

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“…The obtained results showed excellent consistency with previously reported studies by Panga et al . , Modi et al . , and Vine et al .…”

Section: Resultsmentioning

confidence: 95%

Design, Synthesis, Characterization, and In Vitro Evaluation of Isatin‐Pomalidomide Hybrids for Cytotoxicity against Multiple Myeloma Cell Lines

Panga

Podila²,

Veeresham

2018

Journal of Heterocyclic Chem

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in Wiley Online Library (wileyonlinelibrary.com).Inspired by the concept of molecular hybridization, a series of new isatin-pomalidomide hybrids (9a-9g) were designed, synthesized, characterized, and evaluated for in vitro cytotoxic activity against U266B1 and RPMI 8226 multiple myeloma cell lines. Sandmeyer methodology and N-halomethylketo alkylation reaction are the two important reactions involved in the synthesis of isatin-pomalidomide hybrids (9a-9g). All the synthesized compounds (3a-3d, 4, 5, 6, and 9a-9g) were characterized by using IR, mass, 1 H-NMR, and 13 C-NMR spectral techniques. The efficacy of all the synthesized compounds was tested against the aforementioned cell lines by employing MTT assay (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) standard protocols while using pomalidomide as a standard. The test concentrations used in the MTT assay were 1, 10, 20, 30, and 40 μM, and the period of incubation was 24 h. All the synthesized compounds were found to have moderate to greater cytotoxic activity against the aforementioned cell lines. Among them, synthesized hybrids 9f (IC 50 , U266B1 = 5.15 ± 0.72 μM, RPMI8226 = 11.66 ± 0.79 μM) and 9g (IC 50 , U266B1 = 2.50 ± 0.37 μM, RPMI8226 = 6.70 ± 0.55 μM) displayed better cytotoxic activity against both the cell lines used in the present study.

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“…The synthesized compounds showed good anticancer activity towards both the cells. Compound 148 showed the highest activity towards both cell lines having IC 50 values of 9.28 and 14.89 µM and Vinblastine was used as positive control here with IC 50 values of 4.02 and 7.14 µM, respectively [ 262 ]. Eldehna et al (2021) synthesized isatin-thiazolo benzimidazole derivatives and evaluated their cytotoxic activity against MDA-MB-231 and MCF-7 breast cancer cell lines by using sulforhodamine B colorimetric (SRB) assay.…”

Section: Current Advances In Nitrogen Containing Heterocycles As Anti...mentioning

confidence: 99%

Nitrogen Containing Heterocycles as Anticancer Agents: A Medicinal Chemistry Perspective

et al. 2023

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Cancer is one of the major healthcare challenges across the globe. Several anticancer drugs are available on the market but they either lack specificity or have poor safety, severe side effects, and suffer from resistance. So, there is a dire need to develop safer and target-specific anticancer drugs. More than 85% of all physiologically active pharmaceuticals are heterocycles or contain at least one heteroatom. Nitrogen heterocycles constituting the most common heterocyclic framework. In this study, we have compiled the FDA approved heterocyclic drugs with nitrogen atoms and their pharmacological properties. Moreover, we have reported nitrogen containing heterocycles, including pyrimidine, quinolone, carbazole, pyridine, imidazole, benzimidazole, triazole, β-lactam, indole, pyrazole, quinazoline, quinoxaline, isatin, pyrrolo-benzodiazepines, and pyrido[2,3-d]pyrimidines, which are used in the treatment of different types of cancer, concurrently covering the biochemical mechanisms of action and cellular targets.

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Synthesis and anticancer activity of new isatin-benzoic acid conjugates

Cited by 5 publications

References 0 publications

Concept of Hybrid Drugs and Recent Advancements in Anticancer Hybrids

Concept of Hybrid Drugs and Recent Advancements in Anticancer Hybrids

Design, Synthesis, Characterization, and In Vitro Evaluation of Isatin‐Pomalidomide Hybrids for Cytotoxicity against Multiple Myeloma Cell Lines

Nitrogen Containing Heterocycles as Anticancer Agents: A Medicinal Chemistry Perspective

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