Supplimentary Information.docx (3 MB)

Tetrahydroquinoline: an efficient scaffold as mTOR inhibitor for the treatment of lung cancer - Supplementary Information.docx

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posted on 2022-12-20, 15:48 authored by Udit Chaube, Rajdeep Dey, Suman Shaw, Bhumika D Patel, Hardik G Bhatt

Figure SF 01

Lung cancer and its classification

Figure SF 02

Structure of mTOR backbone, which consists of six region the HEAT, FAT (domain focal adhesion targeting domain), FRB (FKBP12 rapamycin binding), KIN (kinase, the target of ATP competitive inhibitors), NRD, and FATC (focal adhesion targeting domain of C-terminal). & Structures of mTORC1 (mTOR complex)1/2. mTORC1 which contains of the mTOR backbone, Raptor, Deptor, mLST8, PRAS40, and mTORC2, which contains of mTOR backbone, Protor, Rictor, Deptor, mSlN1, and mLST8.

Figure SF 03

Structure of some “nib” group of molecules like some EGFR inhibitors viz. 29. Erlotinib & 30. Gifitinib, a tyrosine kinase inhibitor 31. Neratinib, a MEK kinase inhibitor 32. Selumetinib, 33. Cobimetinib/GDC-0973, an ERK inhibitor 34. Trametinib all are used to treat lung cancers.

Figure SF 04

Timeline indicates tetrahydroquinoline derivatives either as a mTOR inhibitor or for the treatment of lung cancer in last ten years.

Table ST 01

Some known mTOR inhibitors