Synthesis of new para-aminobenzoic acid derivatives, in vitro biological evaluation and preclinical validation of DAB-2-28 as a therapeutic option for the treatment of bladder cancer

Oufqir, Yassine; Fortin, Laurie; Girouard, Julie; Cloutier, Francis; Cloutier, Maude; Leclerc, Marie-France; Belgorosky, Denise; Eiján, Ana María; Bérubé, Gervais; Reyes‐Moreno, Carlos

doi:10.1016/j.ejmcr.2022.100069

Cited by 3 publications

(4 citation statements)

References 23 publications

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“…Cyclization was performed to give a targeted reported compound after the hydrolysis of a mixed anhydride intermediate. Lastly, an acid was activated with iso-butyl chloroformate and further treated with tertbutyl carbamate to obtain the required anti-inflammatory derivative [102]. 2-chloroethylamino benzamide was prepared using 4-aminobenzoic acid as starting material.…”

Section: Synthesis Of Anti-inflammatory Agentsmentioning

confidence: 99%

“…Data from in vitro anti-inflammatory and antiproliferative activity disclosed that, among the molecules under study, the derivative of PABA (DAB-2-28) possesses lesser cytotoxic activity with higher efficiency [102]. An enzymatic activity inhibition assay performance against compounds unveiled that the benzamide-derived compound showed good results with IC 50 values of 95.2, 260.7, and 255.7 nM against histone deacetylases (HDAC1, HDAC2, and HDAC3, respectively), while its antiproliferative assay expressed an IC 50 of 2.66 µM (10.3 times) and 1.73 µM (11.3 times), showing greater efficacy than suberoylanilide hydroxamic acid [103].…”

Section: Anti-inflammatory Activitiesmentioning

confidence: 99%

“…Synthetic routes of p-aminobenzoic acid derivatives having anti-inflammatory potential (adapted from ref [102][103][104][106][107][108]…”

mentioning

confidence: 99%

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Novel Para-Aminobenzoic Acid Analogs and Their Potential Therapeutic Applications

Haroon,

Farwa,

Arif

et al. 2023

Biomedicines

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A “building block” is a key component that plays a substantial and critical function in the pharmaceutical research and development industry. Given its structural versatility and ability to undergo substitutions at both the amino and carboxyl groups, para-aminobenzoic acid (PABA) is a commonly used building block in pharmaceuticals. Therefore, it is great for the development of a wide range of novel molecules with potential medical applications. Anticancer, anti-Alzheimer’s, antibacterial, antiviral, antioxidant, and anti-inflammatory properties have been observed in PABA compounds, suggesting their potential as therapeutic agents in future clinical trials. PABA-based therapeutic chemicals as molecular targets and their usage in biological processes are the primary focus of this review study. PABA’s unique features make it a strong candidate for inclusion in a massive chemical database of molecules having drug-like effects. Based on the current literature, further investigation is needed to evaluate the safety and efficacy of PABA derivatives in clinical investigations and better understand the specific mechanism of action revealed by these compounds.

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Section: Synthesis Of Anti-inflammatory Agentsmentioning

confidence: 99%

Section: Anti-inflammatory Activitiesmentioning

confidence: 99%

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Novel Para-Aminobenzoic Acid Analogs and Their Potential Therapeutic Applications

Haroon,

Farwa,

Arif

et al. 2023

Biomedicines

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“…Derivatives of p-amino benzoic acid, 43,44 N-substituted orthoaminobenzoic acid, 45 N-methyl substituted p-aminobenzoic acid 46 are reported to have potential anticancer activities. Aloe-vera is a well-known herb known for its antimicrobial, antioxidant, anti-inflammatory, and anticancer activities.…”

Section: Antioxidant Activitymentioning

confidence: 99%

Anticancer potential of poly(2-aminobenzoic acid)-blend-Aloe vera against the human breast cancer cell line MDA-MB-231

Sebastian¹,

Mary

2022

Journal of Bioactive and Compatible Polymers

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Breast cancer in women is amongst the most significant concerns from time immemorial in the field of oncology. This study proposes an anticancerous polymeric material based on an electroactive substituted polyaniline blend, poly(2-aminobenzoic acid)-blend-Aloe vera (PABA/AV) synthesized by the emulsion polymerization method. The structural, thermal, and morphological characteristics determined using FT-IR and UV-Visible Spectroscopy, XRD, TGA, DTA, and SEM-EDX validated the thermally stable, semi-crystalline, emeraldine salt structure. The material is semi-conducting, and the electrical conductivity measured is 1.86 × 10−3 S/cm. It shows bactericidal efficacy against Enterococcus faecalis at a minimum inhibitory and minimum bactericidal concentration of 50 μg/mL. The radical cations in the emeraldine polymer chain reduce the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical and exhibit a significant % of DPPH scavenging (89.85%) at 20 μL. The polymer blend is active against the human breast cancer cell line MDA-MB-231 and causes 78.65% cytotoxicity at a concentration of 125 μg/mL. The synergistic effect of the ancient healing Aloe vera plant and the electroactive biocompatible poly(2-aminobenzoic acid) certainly opens up new developments in the field of cancer therapy.

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Synthesis, structure, Hirshfeld surface analysis, and molecular docking studies of the Cu(II) complex with 3-nitro-4-aminobenzoic acid

Narmanova,

Turaev,

Kasimov

et al. 2024

Struct Chem

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Synthesis of new para-aminobenzoic acid derivatives, in vitro biological evaluation and preclinical validation of DAB-2-28 as a therapeutic option for the treatment of bladder cancer

Cited by 3 publications

References 23 publications

Novel Para-Aminobenzoic Acid Analogs and Their Potential Therapeutic Applications

Novel Para-Aminobenzoic Acid Analogs and Their Potential Therapeutic Applications

Anticancer potential of poly(2-aminobenzoic acid)-blend-Aloe vera against the human breast cancer cell line MDA-MB-231

Synthesis, structure, Hirshfeld surface analysis, and molecular docking studies of the Cu(II) complex with 3-nitro-4-aminobenzoic acid

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