2-(4-Bromobenzyl) tethered 4-amino aryl/alkyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidines: design, synthesis, anticancer assessment via dual topoisomerase-I/II inhibition, and in silico studies

Sahil Arora, Bhagyshree Patra, Isha Dhamija, Santosh Kumar Guru and Raj Kumar

RSC Med. Chem., 2025,16, 907-926

Abstract

The design, synthesis, and anticancer evaluation via topoisomerase inhibition of 2-(4-bromobenzyl) tethered 4-amino aryl/alkyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidines are reported.

Reinvestigation of diphenylmethylpiperazine analogues of pyrazine as new class of Plasmodial cysteine protease inhibitors for the treatment of malaria

Hari Madhav, G. Srinivas Reddy, Zeba Rizvi, Ehtesham Jameel, Tarosh S. Patel, Abdur Rahman, Vikas Yadav, Sadaf Fatima, Fatima Heyat, Kavita Pal, Amisha Minju-OP, Naidu Subbarao, Souvik Bhattacharjee, Bharat C. Dixit, Puran Singh Sijwali and Nasimul Hoda

RSC Med. Chem., 2024,15, 1022-1037

Abstract

The present study unveils a thorough reevaluation of diphenylmethylpiperazine and pyrazine-derived molecular hybrids, introducing them as a new class of antimalarials.

Naphthyl bearing 1,3,4-thiadiazoleacetamides targeting the parasitic folate pathway as anti-infectious agents: in silico, synthesis, and biological approach

Kavita Pal, Sahil Lala, Priyanka Agarwal, Tarosh S. Patel, Jenny Legac, Md. Ataur Rahman, Saiema Ahmedi, Nida Shahid, Sneha Singh, Kajal Kumari, Hari Madhav, Abhik Sen, Nikhat Manzoor, Bharat C. Dixit, Robyn Van Zyl, Philip J. Rosenthal and Nasimul Hoda

RSC Med. Chem., 2023,14, 2768-2781

Abstract

Naphthyl bearing 1,3,4-thiadiazoleacetamides targeting the parasitic folate pathway as antimalarials and antileishmanial agents.

Design and preparation of a new Ni/Arg@zeolite-Y nano-composite: investigation of its performance as a multi-functional and bio-organic catalyst for the one-pot synthesis of thieno[2,3-d]pyrimidinones

Mehdi Kalhor, Ziba Modares and Vahid Azizkhani

RSC Adv., 2025,15, 28045-28062

Abstract

This paper describes the design and fabrication of a Ni/Arg@zeolite-Y nanocomposite, and investigates its application as a multifunctional nanocatalyst in the one-pot synthesis of thieno[2,3-d]pyrimidinone derivatives.

Sulfonamide based pyrimidine derivatives combating Plasmodium parasite by inhibiting falcipains-2 and falcipains-3 as antimalarial agents

Abdur Rahman, Shazia Anjum, Jaimin D. Bhatt, Bharat C. Dixit, Anju Singh, Sabiha khan, Sadaf Fatima, Tarosh S. Patel and Nasimul Hoda

RSC Adv., 2024,14, 24725-24740

Abstract

In this report, we present the design and synthesis of a novel series of pyrimidine-tethered spirochromane-based sulfonamide derivatives aimed at combating drug resistance in malaria.